Prof. Steven Ballet
Fluorinated Peptide Hydrogels Result in Longer In Vivo Residence Time after Subcutaneous Administration
Honfroy, A., Bertouille, J., Turea, A., Cauwenbergh, T., Bridoux, J., Lensen, M., Mangialetto, J., Van den Brande, N., White, J., Gardiner, J., Brigaud, T., Ballet, S., Hernot, S., Chaume, G., Martin, D., DOI: 10.1021/acs.biomac.4c00872Design, Synthesis, and In Vitro Characterization of Proteolytically-Stable Opioid-Neurotensin Hybrid Peptidomimetics
De Neve, J., Breault, E., Previti, S., Vangeloven, E., Loranger, B., Chartier, M., Brouillette, R., Lanoie, A., Holleran, BJ., Longpré, JM., Gendron, L., Tourwé, D., Sarret, P., Ballet, S., doi 10.1021/acsptsci.4c00236 pubs.acs.org/ptsci...Allosteric nanobodies to study the interactions between SOS1 and RAS
Fischer, B., Uchański, T., Sheryazdanova, A., Gonzalez, S., Volkov, A., Brosens, E., Zögg, T., Kalichuk V., Ballet, S., Versées, W., Sablina, A., Pardon, E., Wohlkönig, A., Steyaert, J., Nat Commun. 2024 Jul 23;15(1):6214.Peptide libraries: from epitope mapping to in-depth high-throughput analysis.
Laculli, D., Ballet, S., Sciencedirect Volume 45, Issue 7 , July 2024, Pages 579-582Multitarget µ-opioid receptor agonists-neuropeptide FF receptor antagonists induce potent antinociception with reduced adverse side effects.
De Neve, J.; Elhabazi, K.§; Gonzalez, S.; Herby, C.; Schneider, S.; Utard, V.; Fellmann-Clauss, R.; Petit-Demouliere, N.; Lecat, S.; Kremer, M.; Ces, A.; Daubeuf, F.; Martin, C.; Ballet, S.; Bihel, F.; Simonin, F., J Med Chem. 2024 May 9;67(9):7603-7619.Peptide Sequence Variations Govern Hydrogel Stiffness: Insights from a Multi-Scale Structural Analysis of H-FQFQFK-NH2 Peptide Derivatives
T. De Maeseneer, T. Cauwenbergh, J. Gardiner, J. F. White, W. Thielemans, C. Martin, P. Moldenaers, S. Ballet, R. Cardinaels, Macromol Biosci. 2024 Mar 29:e2300579.Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design
Luis E. Gimenez, C. Martin, J. Yu, C. Hollanders, Ciria C. Hernandez, Y. Wu, D. Yao,G. Won Han, Naima S. Dahir, L. Wu, O. Van der Poorten, A. Lamouroux, M. Mannes, S. Zhao, D. Tourwé, RC. Stevens, RD. Cone, S. Ballet, J. Med. Chem. 2024, 67, 4, 2690–2711Sustained release of a human PD-L1 single-domain antibody using peptide-based hydrogels
Heremans, J., Maximilian Awad, R., Bridoux, J., Ertveldt, T., Caveliers V., Madder A., Hoogenboom R., Devoogdt N., Ballet S., Hernot S., Breckpot K., Martin C., Eur J Pharm Biopharm 2024 Mar:196:114183. .Structure-Based Design and Synthesis of Stapled 10Panx1 Analogues for Use in Cardiovascular Inflammatory Diseases
Lamouroux, A.; Tournier, M.; Iaculli, D.; Caufriez, A.; Rusiecka, O.M.; Martin, C.; Bes, V.; Carpio, L.E.; Girardin, Y.; Loris, R.; Tabernilla, A.; Molica, F.; Gozalbes, R.; Mayán, M.D.; Vinken, M.; Kwak, B.R.; Ballet, S.; J. Med. Chem. 2023, 66, 18, 13086–13102Smart hydrogels delivered by high pressure aerosolization can prevent peritoneal adhesions
Braet, H.; Fransen, P.-P.; Chen, Y.; Van Herck, S.; Mariën, R.; Vanhoorne, V.; Ceelen, W.; Madder, A.; Ballet, S.; Hoogenboom, R.; De Geest, B.; Hoorens, A.; Dankers, P.Y.W.; De Smedt, S.C.; Remaut, K.; J. Control Release, 2023, 362, 138-150Identification of small molecule antivirals against HTLV-1 by targeting the hDLG1-Tax-1 protein-protein interaction
Maseko, S.B.; Brammerloo, Y.; Van Molle, I.; Sogues, A.; Martin, C.; Gorgulla, C.; Plant, E.; Olivet, J.; Blavier, J.; Ntombela, T.; Delvigne, F.; Arthanari, H.; El Hajj, H.; Bazarbachi, A.; Van Lint, C.; Salehi-Ashtiani, K.; Remaut, H.; Ballet, S.; Volkov, A.N.; Twizere, J-C.; Antiviral Research, 2Introduction of constrained Trp analogs in RW9 modulates structure and partition in membrane models
Lozada, C.; Simon Gonzalez, S.; Agniel, R.; Hindie, M.; Manciocchi, L.; Mazzanti, L.; Ha-Duong, T.; Federica Santoro, F.; Carotenuto, A.; Ballet, S.; Lubin-Germain, N.; Bioorganic chemistry, 2023, 139, 106731Bypassing the Need for Cell Permeabilization: Nanobody CDR3 Peptide Improves Binding on Living Bacteria
Breine, A.; Van holsbeeck, K.; Martin, C.; Gonzalez, S.; Mannes, M.; Pardon, E.; Steyaert, J.; Remaut, H.; Ballet, S.; Van der Henst, C.; Bioconjugate Chem. 2023, 34, 7, 1234-1243Determination of structural features that underpin the pannexin1 channel inhibitory activity of the peptide 10Panx1
Caufriez, A.; Lamouroux, A.; Martin, C.; Iaculli, D.; Ergüç, EI.; Gozalbes, R.; Mayan, M.D.; Kwak, B.R.; Tabernilla, A.; Vinken, M.; Ballet, S., Bioorg. Chem. 2023 DOI: 10.1016/j.bioorg.2023.106612Nanobody Loop Mimetics Enhance Son of Sevenless 1-Catalyzed Nucleotide Exchange on RAS
Van holsbeeck, K., Fischer, B., Gonzalez, S., Gadais, C., Versées, W., Martins, J. C., Martin, C., Wohlkönig, A., Steyaert, J., Ballet, S., Angew. Chem. Int. Ed. 2023, e202219095; Angew. Chem. 2023, e202219095.Nature-Inspired Dual Purpose Strategy toward Cell-Adhesive PCL Networks: C(-linker-)RGD Incorporation via Thiol-ene Crosslinking
Thijssen, Q., Parmentier, L., Van Holsbeeck, K., Ballet, S. and Van Vlierberghe, S. Biomacromolecules 2023, 24(4), 1638-1647.Fast Self-Assembly Dynamics of a β-Sheet Peptide Soft Material
J. Bertouille, S. Kasas, C. Martin, U. Hennecke, S. Ballet, R. Willaert, R. G., Small, 2023, 2206795.Signaling Modulation via Minimal C‑Terminal Modifications of Apelin-13
Théroux, L.; Van Den Hauwe, R.; Trân, K.; Fournier, J.; Desgagné, M.; Meneboo, N.; Lavallée, A.; Fröhlich, U.; Côté, J.; Hollanders, C.; Longpré, J-M.; Murza, A.; Marsault, E.; Philippe Sarret, P.; Boudreault, P-L.; Ballet, S., ACS Pharmacol. Transl. Sci. 2023, DOI 10.1021/acsptsci.2c00219Second generation Spautin-1 analogues targeting EGFR-mutant non-small cell lung cancer cells
Elsocht, M., Giron, P., De Grève, J., Ballet, S. Bioorg. Med. Chem Lett. 2023, 79, 129066.Propargylamine Amino Acids as Constrained Nε‑Substituted Lysine Mimetics
Herein, alkylated propargylamines are reported as constrained lysine mimetics and constructed in a single step using a copper(I)-catalyzed A3-coupling reaction.Opening the amino acid toolbox for peptide-based NTS2-selective ligands as promising lead compounds for pain management
Chronic pain is one of the most critical health issues worldwide. Despite considerable efforts to find therapeutic alternatives, opioid drugs remain the gold standard for pain management.Bifunctional Peptidomimetic G Protein-Biased Mu-Opioid Receptor Agonist and Neuropeptide FF Receptor Antagonist KGFF09 Shows Efficacy in Visceral Pain without Rewarding Effects after Subcutaneous Administration in Mice
There is still an unmet clinical need to develop new pharmaceuticals for effective and safe pain management. Current pharmacotherapy offers unsatisfactory solutions due to serious side effects related to the chronic use of opioid drugs.Impact of doubling peptide length on in vivo hydrogel stability and sustained drug release
Heremans, J., Chevillard, L., Mannes, M., Mangialetto, J., Leroy, K., White, J.F., Lamouroux, A., Vinken, M., Gardiner, J., Van Mele, B. and Van den Brande, N., Hoogenboom, R., Madder, A., Caveliers, V., Mégarbane, B., Hernot, S., Ballet, S., Martin, C., J. Controlled Release, 2022, 350, 514-524.A Quantum Chemical Deep-Dive into the pi-pi Interactions of 3-Methylindole and Its Halogenated Derivatives—Towards an Improved Ligand Design and Tryptophan Stacking
Van Lommel, R.; Bettens, T.; Barlow, T.M.A.; Bertouille, J.; Ballet, S.; De Proft, F. Pharmaceuticals 2022, 15, 935. https://doi.org/10.3390/ph15080935Wandering beyond small molecules: peptides as allosteric protein modulators
Mannes, M.; Martin, C.; Menet, C.; Ballet, S. Trends Pharmacol. Sci. 2021, , 43(5), 406-423Antimicrobial Activity of a Repurposed Harmine-Derived Compound on Carbapenem- Resistant Acinetobacter baumannii Clinical Isolates
Breine, A.; Van Gysel, M.; Elsocht, M.; Whiteway, C.; Philippe, C.; Quinet, T.; Valcek, A.; Wouters, J.; Ballet, S.; Van der Henst,. C.; Front. Cell. Infect. Microbiol. 2022, 11:789672.; doi: https://doi.org/10.1101/2021.06.30.45046Genome-based characterization of a plasmid-associated micrococcin P1 biosynthetic gene cluster and virulence factors in Mammaliicoccus sciuri IMDO-S72
Van der Veken, D.; Hollanders, C.; Verce, M.; Michiels, C.; Ballet, S.; Weckx, S.; Leroy, F. Applied and environmental microbiology, 2021, AEM-02088. DOI:10.1128/AEM.02088-21Downsizing antibodies: Towards complementarity-determining region (CDR)-based peptide mimetics
Monoclonal antibodies emerged as an important therapeutic drug class with remarkable specificity and binding affinity.Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional mu/delta-Opioid Agonist–Neurokinin Antagonist Peptidomimetics
Opioid agonists are well-established analgesics, widely prescribed for acute but also chronic pain. However, their efficiency comes with the price of drastically impacting side effects that are inherently linked to their prolonged use.Identification and Characteristics of Fusion Peptides Derived From Enveloped Viruses
Lozada, C.; Barlow, T. M. A.; Gonzalez, S.; Lubin-Germain, N.; Ballet, S. Frontiers Chemistry (Chemical Biology) 2021, 9, 689006Neuromedin U induces an invasive phenotype in CRC cells expressing the NMUR2 receptor
Successful colorectal cancer (CRC) therapy often depends on the accurate identification of primary tumours with invasive potential. There is still a lack of identified pathological factors associated with disease recurrence that could help in making treatment decisions.Harnessing the anti-nociceptive potential of NK2 and NK3 ligands in the design of new multifunctional µ/δ-opioid agonist-neurokinin antagonist peptidomimetics.
Gadais, C.; Piekielna-Ciesielska, J.; De Neve, J.; Martin, C.; Janecka, A.; Ballet, S.Efficient Synthesis of Polysubstituted 1,5-Benzodiazepinone Dipeptide Mimetics via an Ugi-4CR-Ullmann Condensation Sequence
An efficient three-step synthesis towards 3-amino-1,4-benzodiazepin-2-one derivatives is presented. The versatile Ugi-4-component reaction (Ugi-4CR) and Boc deprotection is followed by a ligand-free Ullmann condensation.Towards the understanding of halogenation in peptide hydrogels: a quantum chemical approach.
Bettens, T.; Lacanau, V.; Van Lommel, R.; De Maeseneer, T.; Vandeplassche, W.; Brancart, J.; Barlow, T.; Woller, T. M.; Van den Brande, N.; Moldenaers, P.; De Proft, F.; Madder, A.; Hoogenboom, R.; Martin, C.; Ballet, S.; Alonso Giner, M. Materials Advances, 2021 2(14), 4792-4803.3-Substituted 2-isocyanopyridines as versatile convertible isocyanides for peptidomimetic design
Hollanders, C.; Elsocht, M.; Van der Poorten, O.; Jida, M.; Renders, E.; Maes, B.U.W.; Ballet, S. Chem Comm, 2021, DOI: 10.1039/D1CC01701B...Antinociceptive Efficacy of the μ‐Opioid/Nociceptin Peptide‐Based Hybrid KGNOP1 in Inflammatory Pain without Rewarding Effects in Mice: An Experimental Assessment and Molecular Docking
Dumitrascuta, M.; Bermudez, M.; Trovato, O.; Neve, J.D.; Ballet, S.; Wolber, G.; Spetea, M., Molecules 2021, 26, 3267.Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability
Tourwé, D.; Tsiailanis, A. D.; Parisis, N.; Hirmiz, B.; Del Borgo, M.; Aguilar, M.-I.; Van der Poorten, O.; Ballet, S.; Widdop, R. E.;Tzakos, A. G., Bioorg. Med. Chem. Lett, 2021, 43, 128086.Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors
De Neve, J.; Barlow, T. M.; Tourwé, D.; Bihel, F.; Simonin, F.; Ballet, S., RSC Med. Chem., 2021 DIO: 10.1039/D1MD00041A...Antinociceptive Efficacy of the µ-Opioid/Nociceptin Peptide-Based Hybrid KGNOP1 in Inflammatory Pain without Rewarding Effects in Mice: An Experimental Assessment and Molecular Docking
Dumitrascuta, M.; Bermudez, M.; Trovato, O.; De Neve, J.; Ballet, S.; Wolber, G.; Spetea, M.Development of Generic G Protein Peptidomimetics Able to Stabilize Active State Gs Protein‐Coupled Receptors for Application in Drug Discovery
Mannes, M.; Martin, C.; Triest, S.; Pia Dimmito, M.; Mollica, A.; Laeremans, T.; Menet, C.J.; Ballet, S., Angew. Chem. Int. Ed. 2021. https://doi.org/10.1002/anie.202100180Constraining the Side Chain of C‑Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile
Trân, K.; Van Den Hauwe, R.; Sainsily, X.; Couvineau, P.; Côté, J.; Simard, L.; Echevarria, M.; Murza, A.; Serre, A.; Théroux, L.; Saibi, S.; Haroune, L.; Longpré, J-M.; Lesur, O.; Auger-Messier, M.; Spino, C.; Bouvier, M.; Sarret, P.; Ballet, S.; Marsault, E.; J. Med. Chem., ASAP...Structure–Activity Relationship (SAR) Study of Spautin-1 to Entail the Discovery of Novel NEK4 Inhibitors
Elsocht, M.; Giron, P.; Maes, L.; Wim Versées. W.; Gutierrez, G.J.; De Grève, J.; Ballet S.; Int. J. Mol. Sci. 2021, 22(2), 635Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure
Martin, C.; Gimenez, L. E.; Williams, S. Y.; Jing, Y.; Wu, Y.; Hollanders, C.; Van der Poorten, O.; Gonzalez, S.; Van holsbeeck, K.; Previti, S.; Lamouroux, A.; Zhao, S.; Tourwé, D.; Stevens R.C.; Cone R.D.; Ballet, S., J. Med. Chem. 2021, 64, 1, 357–369Anti-human PD-L1 Nanobody for Immuno-PET Imaging: Validation of a Conjugation Strategy for Clinical Translation
Bridoux, J.; Broos, K.; Lecocq, Q.; Debie, P.; Martin, C.; Ballet, S.; Raes, G.; Neyt, S.; Vanhove, C.; Breckpot, K.; Devoogdt, N.; Caveliers, V.; Keyaerts, M.; Xavier, C.; Biomolecules, 2020, 10(10), 1388.Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies
Gonzalez, S.; Dumitrascuta, M.; Eiselt, E.; Louis, S.; Kunze, L.; Blasiol, A.; Vivancos, M.; Previti,S.; Dewolf, E.; Martin, C.; Tourwé, D.; Cavelier, F.; Gendron, L.; Sarret, P.; Spetea, M.; Ballet, S.; J. Med. Chem. 2020, 63, 21, 12929–12941Peptide-based targeting of connexins and pannexins for therapeutic purposes
Caufriez, A;, Böck, D.; Martin, C.; Ballet, S.; Vinken, M.; Expert Opinion on Drug Discovery, 2020, 15(10), 1213-1222.Insightful Backbone Modifications Preventing Proteolytic Degradation of Neurotensin Analogs Improve NTS1-Induced Protective Hypothermia
Previti, S.; Vivancos, M.; Rémond, E.; Beaulieu, S.; Longpré, J. M.; Ballet, S.; Sarret, P.; Cavelier, F.; Frontiers in Chemistry, 2020, 8, 406Mechanistic Understanding of Peptide Analogues, DALDA, [Dmt1]DALDA, and KGOP01, Binding to the Mu Opioid Receptor
Dumitrascuta, M.; Bermudez, M.; Ballet, S., Wolber, G.; Spetea, M. Molecules, 2020, 25(9), 2087.Effects of neuromedin U-8 on stress responsiveness and hypothalamus-pituitary-adrenal axis activity in male C57BL/6J mice.
De Prins A.; Allaoui W.; Medrano M.; Van Eeckhaut A.; Ballet S.; Smolders I.; De Bundel D. Hormones and Behavior, 2020, 121, 104666.The Neurokinins: Peptidomimetic Ligand Design and Therapeutic Applications
Gadais, C.; Ballet, S. Current medicinal chemistry, 2020, 27(9), 1515-1561.A New Family of Diverse Skin Peptides from the Microhylid Frog Genus Phrynomantis
Raaymakers, C.; Stijlemans, B.; Martin, C.; Zaman, S.; Ballet, S.; Martel, A.; Pasmans, F.; Roelants, K. Molecules 2020, 25(4), 912Zn-Catalyzed Nicotinate-Directed Transamidations in Peptide Synthesis
Hollanders, C.; Renders, E.; Gadais, C.; Masullo, D.; Van Raemdonck, L.; Wybon, C. C. D.; Martin, C.; Herrebout, W. A.; Maes, B. U. W.; Ballet, S. ACS Catal., 2020 DOI: 10.1021/acscatal.9b05074Primary Hepatocytes and Their Cultures for the Testing of Drug-Induced Liver Injury.
Vilas-Boas, V.; Cooreman, A.; Gijbels, E.; Van Campenhout, R.; Gustafson, E.; Ballet, S.; Annaert, P.; Cogliati, B.; Vinken, M., Advances in Pharmacology 2019, 85, 1-30.Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists.
Claff, T.; Yu, J.; Blais, V.; Patel, N.; Martin, C.; Wu, L.; Han, G. W.; Holleran, B. J.; Van der Poorten, O.; White, K. L.; Hanson, M. A.; Sarret, P.; Gendron, L.; Cherezov, V.; Katritch, V.; Ballet, S.; Liu, Z.-J.; Müller, C. E.; Stevens, R. C., Sci. Adv 2019, 5, eaax9115.Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia.
Eiselt, E.; Gonzalez, S.; Martin, C.; Chartier, M.; Betti, C.; Longpré, J.-M.; Cavelier, F.; Tourwé, D.; Gendron, L.; Ballet, S.; Sarret, P., ACS Chem. Neurosci. 2019, 10, 4535-4544.Neuromedin U and Structural Analogs: an Overview of Their Structure, Function and Selectivity
De Prins A.; Van Eeckhaut A.; Smolders I.; Tourwé D.; Ballet S. Curr. Med. Chem. 2019, 26, 1.The 1,3-diyne linker as a rigid "i,i+7" staple for alpha-helix stabilization: Stereochemistry at work.
Verlinden, S.; Geudens, N.; Van holsbeeck, K.; Mannes, M.; Martins, J. C.; Verniest, G.; Ballet, S., J. Pept. Sci. 2019, 25, e3194Solid-Phase Azopeptide Diels-Alder Chemistry for Aza-pipecolyl Residue Synthesis To Study Peptide Conformation.
Chingle, R.; Mulumba, M.; Chung, N. N.; Nguyen, T. M. D.; Ong, H.; Ballet, S.; Schiller, P. W.; Lubell, W. D., J. Org. Chem. 2019, 84, 6006-6016.Trifluoromethylated Proline Surrogates as Part of “Pro–Pro” Turn-Inducing Templates.
Gadais, C.; Van holsbeeck, K.; Moors, S. L. C.; Buyst, D.; Fehér, K.; Van Hecke, K.; Tourwé, D.; Brigaud, T.; Martin, C.; De Proft, F.; Pytkowicz, J.; Martins, J. C.; Chaume, G.; Ballet, S., ChemBioChem 2019, 20, 2513-2518.Connexin and pannexin (hemi)channels: emerging targets in the treatment of liver disease.
Cooreman, A.; van Campenhout, R.; Ballet, S.; Annaert, P.; Van Den Bossche, B.; Colle, I.; Cogliati, B.; Vinken, M., Hepatology 2019, 69, 1317-1323Radiometal-labeled anti-VCAM-1 nanobodies as molecular tracers for atherosclerosis – impact of radiochemistry on pharmacokinetics.
Bala, G.; Crauwels, M.; Blykers, A.; Remory, I.; Marschall Andrea, L. J.; Dübel, S.; Dumas, L.; Broisat, A.; Martin, C.; Ballet, S.; Cosyns, B.; Caveliers, V.; Devoogdt, N.; Xavier, C.; Hernot, S., Biol. Chem., 2019; 400, 323.Primary Hepatocytes and Their Cultures for the Testing of Drug-Induced Liver Injury.
Vilas-Boas, V.; Cooreman, A.; Gijbels, E.; Van Campenhout, R.; Gustafson, E.; Ballet, S.; Annaert, P.; Cogliati, B.; Vinken, M., Advances in Pharmacology 2019, 85, 1-30.Modulating peptide hydrogel strength through halogenation.
Vandeplassche, W.; Ballet, S.; Martin, C.; Hoogenboom, R.; Madder, A., J. Pept. Sci. 2018, 24, S109-S110.Design, synthesis and biological evaluation of stapled helical peptides targeting the myddosome.
Terriers, V.; Verhoeven, J.; Martin, C.; Hollanders, K.; Triballeau, N.; Mollat, P.; Van der Plas, S.; De Wilde, G.; Ballet, S., J. Pept. Sci. 2018, 24, S157-S157.A Bifunctional Biased Mu Opioid Agonist - Neuropeptide FF Receptor Antagonist as Analgesic with Improved Acute and Chronic Side Effects.
la Rochelle, A. D.; Guillemyn, K.; Dumitrascuta, M.; Gonzalez, S.; Martin, C.; Utard, V.; Quillet, R.; Schneider, S.; Daubeuf, F.; Willemse, T.; Mampuys, P.; Maes, B.; Frossard, N.; Bihel, F.; Spetea, M.; Simonin, F.; Ballet, S., J. Pept. Sci. 2018, 24, S156-S156.Trifluoromethylated proline surrogates as part of 'Pro-Pro' turn-inducing templates for the design of beta-hairpin mimetics.
Gadais, C.; Van Holsbeeck, K.; Moors, S.; Feher, K.; Pytkowicz, J.; Martins, J.; De Proft, F.; Tourwe, D.; Brigaud, T.; Martin, C.; Chaume, G.; Ballet, S., J. Pept. Sci. 2018, 24, S117-S117.The Neurokinins: Peptidomimetic Ligand Design and Therapeutic Applications.
Gadais, C.; Ballet, S., Current Medicinal Chemistry 2018, 25, 1-44.Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.
Martin, C.; Dumitrascuta, M.; Mannes, M.; Lantero, A.; Bucher, D.; Walker, K.; Van Wanseele, Y.; Oyen, E.; Hernot, S.; Van Eeckhaut, A.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., J. Med. Chem. 2018, 61, 9784-9789.Site-Specific Radioactive Labeling of Nanobodies.
Crauwels, M.; Massa, S.; Martin, C.; Betti, C.; Ballet, S.; Devoogdt, N.; Xavier, C.; Muyldermans, S. In Antibody Engineering: Methods and Protocols, Nevoltris, D.; Chames, P., Eds. Springer New York: New York, NY, 2018; pp 505-540.A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects.
la Rochelle, A. D.; Guillemyn, K.; Dumitrascuta, M.; Martin, C.; Utard, V.; Quillet, R.; Schneider, S.; Daubeuf, F.; Willemse, T.; Mampuys, P.; Maes, B. U. W.; Frossard, N.; Bihel, F.; Spetea, M.; Simonin, F.; Ballet, S., Pain 2018, 159, 1705-1718.Bromotryptophans and their incorporation in cyclic and bicyclic privileged peptides.
García-Pindado, J.; Willemse, T.; Goss, R.; Maes, B. U. W.; Giralt, E.; Ballet, S.; Teixidó, M., Biopolymers 2018, 109, e23112.Chemical space screening around Phe3 in opioid peptides : Modulating µ versus δ agonism by Suzuki-Miyaura cross-couplings.
Willemse, T.; Eiselt, E.; Hollanders, K.; Schepens, W.; van Vlijmen, H. W. T.; Chung, N. N.; Blais, V.; Holleran, B.; Longpré, J.-M.; Schiller, P. W.; Maes, B. U. W.; Sarret, P.; Gendron, L.; Ballet, S., Bioorg. Med. Chem. Lett. 2018, 28, 2320-2323Nanobody-Enabled Reverse Pharmacology on G-Protein-Coupled Receptors.
Pardon, E.; Betti, C.; Laeremans, T.; Chevillard, F.; Guillemyn, K.; Kolb, P.; Ballet, S.; Steyaert, J., Angew. Chem. Int. Ed. 2018, 57, 5292-5295.Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists.
De Prins, A.; Martin, C.; Van Wanseele, Y.; Tomboly, C.; Tourwe, D.; Caveliers, V.; Holst, B.; Van Eeckhaut, A.; Rosenkilde, M. M.; Smolders, I.; Ballet, S., ACS Med. Chem. Lett 2018, 9, 496-501.Indoloazepinone-Constrained Oligomers as Cell-Penetrating and Blood-Brain-Barrier-Permeating Compounds.
Van der Poorten, O.; Legrand, B.; Vezenkov, L. L.; Garcia-Pindado, J.; Bettache, N.; Knuhtsen, A.; Pedersen, D. S.; Sanchez-Navarro, M.; Martinez, J.; Teixido, M.; Garcia, M.; Tourwe, D.; Amblard, M.; Ballet, S, ChemBioChem 2018, 19, 696-705.Binding-Site Compatible Fragment Growing Applied to the Design of β2-Adrenergic Receptor Ligands.
hevillard, F.; Rimmer, H.; Betti, C.; Pardon, E.; Ballet, S.; van Hilten, N.; Steyaert, J.; Diederich, W. E.; Kolb, P., J. Med. Chem. 2018, 61, 1118-1129.Efficient one-pot synthesis of enantiomerically pure N-protected-alpha-substituted piperazines from readily available alpha-amino acids : N -protected-α-substituted piperazines from readily available α-amino acids.
Jida, M.; Ballet, S., New J. Chem. 2018, 42, 1595-1599.An Efficient One-Pot Synthesis of Chiral N-Protected 3-Substituted (Diketopiperazines via Ugi-4CR/De-Boc/Cyclization Process.
Jida, M.; Ballet, S., ChemistrySelect 2018, 3, 1027-1031.Zn-Catalyzed tert-Butyl Nicotinate-Directed Amide Cleavage as a Biomimic of Metallo-Exopeptidase Activity.
Wybon, C. C. D.; Mensch, C.; Hollanders, C.; Gadais, C.; Herrebout, W. A.; Ballet, S.; Maes, B. U. W., ACS Catalysis 2018, 8, 203-218.Rapid construction of substituted 3-amino-1,5-benzothiazepin-4(5H)-one dipeptide scaffolds through an Ugi-4CR - Ullmann cross-coupling sequence.
Van der Poorten, O.; Van Den Hauwe, R.; Hollanders, K.; Maes, B. U. W.; Tourwe, D.; Jida, M.; Ballet, S., Org. Biomol. Chem. 2018, 16, 1242-1246.Efficient One-Pot Access to Trisubstituted 2-Benzazepin-3-ones as Constrained Pseudopeptide Analogues and Privileged Scaffolds.
Van der Poorten, O.; Jida, M.; Tourwé, D.; Ballet, S., Medicinal Chemistry 2018, 14, 400-408.Development of potent and proteolytically stable human neuromedin U receptor agonists.
De Prins, A.; Martin, C.; Van Wanseele, Y.; Skov, L. J.; Tomboly, C.; Tourwe, D.; Caveliers, V.; Van Eeckhaut, A.; Holst, B.; Rosenkilde, M. M.; Smolders, I.; Ballet, S., Eur. J. Med. Chem. 2018, 144, 887-897.Antimicrobial peptides in frog poisons constitute a molecular toxin delivery system against predators.
Raaymakers, C.; Verbrugghe, E.; Hernot, S.; Hellebuyck, T.; Betti, C.; Peleman, C.; Claeys, M.; Bert, W.; Caveliers, V.; Ballet, S.; Martel, A.; Pasmans, F.; Roelants, K., Nature Communications 2017, 8, 1495χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Van der Poorten, O.; Van Den Hauwe, R.; Eiselt, E.; Betti, C.; Guillemyn, K.; Chung, N. N.; Hallé, F.; Bihel, F.; Schiller, P. W.; Tourwé, D.; Sarret, P.; Gendron, L.; Ballet, S., ACS Medicinal Chemistry Letters 2017, 8, 1177-1182.Cyclisation To Form Small, Medium and Large Rings by Use of Catalysed and Uncatalysed Azide–Alkyne Cycloadditions (AACs).
This microreview briefly summarises recent developments in the cyclisation to form small, medium and large rings (five to 30 or more members) by way of both catalysed and uncatalysed azide–alkyne cycloaddition (AAC).Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice.
Starnowska, J.; Costante, R.; Guillemyn, K.; Popiolek-Barczyk, K.; Chung, N. N.; Lemieux, C.; Keresztes, A.; Van Duppen, J.; Mollica, A.; Streicher, J.; Vanden Broeck, J.; Schiller, P. W.; Tourwé, D.; Mika, J.; Ballet, S.; Przewlocka, B., ACS Chemical Neuroscience 2017, 8, 2315-2324.Rational Design of Nanobody80 Loop Peptidomimetics: Towards Biased beta(2) Adrenergic Receptor Ligands.
Martin, C.; Moors, S. L. C.; Danielsen, M.; Betti, C.; Fabris, C.; Pedersen, D. S.; Pardon, E.; Peyressatre, M.; Feher, K.; Martins, J. C.; Mathiesen, J. M.; Morris, M. C.; Devoogdt, N.; Caveliers, V.; De Proft, F.; Steyaert, J.; Ballet, S., Eur. Chem. J. 2017, 23, 9632-9640.Amine Activation: N-Arylamino Acid Amide Synthesis from Isothioureas and Amino Acids.
Yan‐Ping, Z.; Pieter, M.; Sergey, S.; Steven, B.; W., M. B. U., Adv. Synth. Catal. 2017, 359, 2481-2498.Bifunctional opioid/nociceptin hybrid KGNOP1 effectively attenuates pain related behaviour in a rat model of neuropathy.
Starnowska, J.; Guillemyn, K.; Makuch, W.; Mika, J.; Ballet, S.; Przewlocka, B., Eur. J Pharm. 2017, 104, 221-229.In Vivo Imaging of the Stability and Sustained Cargo Release of an Injectable Amphipathic Peptide-Based Hydrogel.
Oyen, E.; Martin, C.; Caveliers, V.; Madder, A.; Van Mele, B.; Hoogenboom, R.; Hemot, S.; Ballet, S., Biomacromolecules 2017, 18, 994-1001.The Suzuki–Miyaura Cross-Coupling as a Versatile Tool for Peptide Diversification and Cyclization.
Willemse, T.; Schepens, W.; Vlijmen, H.; Maes, B.; Ballet, S., Catalysts 2017, 7, 74.Bifunctional peptide-based opioid agonist/nociceptin antagonist ligand for dual treatment of nociceptive and neuropathic pain.
Lagard, C.; Chevillard, L.; Guillemyn, K.; Risède, P.; Laplanche, J.-L.; Spetea, M.; Ballet, S.; Mégarbane, B., PAIN 2017, 158, 505-515.Injectable peptide-based hydrogel formulations for the extended in vivo release of opioids.
Martin, C.; Oyen, E.; Van Wanseele, Y.; Ben Haddou, T.; Schmidhammer, H.; Andrade, J.; Waddington, L.; Van Eeckhaut, A.; Van Mele, B.; Gardiner, J.; Hoogenboom, R.; Madder, A.; Spetea, M.; Ballet, S., Materials Today Chemistry 2017, 3, 49-59.Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds.
Dyniewicz, J.; Lipiński, P. F. J.; Kosson, P.; Leśniak, A.; Bochyńska-Czyż, M.; Muchowska, A.; Tourwé, D.; Ballet, S.; Misicka, A.; Lipkowski, A. W., ACS Medicinal Chemistry Letters 2017, 8, 73-77.Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.
Van der Poorten, O.; Knuhtsen, A.; Sejer Pedersen, D.; Ballet, S.; Tourwé, D., J. Med. Chem. 2016, 59, 10865-10890.Synthesis of Heterocycle-Bridged Peptidic Macrocycles through 1,3-Diyne Transformations.
Verlinden, S.; Ballet, S.; Verniest, G., Eur. J. Org. Chem. 2016, 2016, 5807-5812.Controlled-release of opioids for improved pain management.
Martin, C.; De Baerdemaeker, A.; Poelaert, J.; Madder, A.; Hoogenboom, R.; Ballet, S., Mater. Today 2016, 19, 491-502.Conformationally Constrained Peptidomimetics as Inhibitors of the Protein Arginine Methyl Transferases.
Knuhtsen, A.; Legrand, B.; Van der Poorten, O.; Amblard, M.; Martinez, J.; Ballet, S.; Kristensen, J. L.; Pedersen, D. S., Chem.: Eur. J 2016, 22, 14022-14028.Sortase A-mediated site-specific labeling of camelid single-domain antibody-fragments : a versatile strategy for multiple molecular imaging modalities.
Massa, S.; Vikani, N.; Betti, C.; Ballet, S.; Vanderhaegen, S.; Steyaert, J.; Descamps, B.; Vanhove, C.; Bunschoten, A.; Leeuwen, F. W. B.; Hernot, S.; Caveliers, V.; Lahoutte, T.; Muyldermans, S.; Xavier, C.; Devoogdt, N., Contrast Media Mol Imaging 2016, 11, 328-339.Towards β-arrestin biased β2AR ligands: Rational Design of Nanobody Loop Mimetics.
Martin, C.; Betti, C.; Fabris, C.; Mathiesen, J. M.; Pardon, E.; Peyressatre, M.; Moors, S.; De Proft, F.; Feher, K.; Martins, J.; Morris, M. C.; Devoogdt, N.; Caveliers, V.; Steyaert, J.; Ballet, S., J. Pept. Sci. 2016, 22, S134-S134.Injectable Peptide Hydrogels for Controlled Drug Release.
Oyen, E.; Martin, C.; Hernot, S.; Gardiner, J.; Van Mele, B.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., J. Pept. Sci. 2016, 22, S84-S84Development of Potent Neuromedin U Receptor Agonists.
De Prins, A.; Martin, C.; Caveliers, V.; Van Eeckhaut, A.; Holst, B.; Smolders, I.; Ballet, S., J. Pept. Sci. 2016, 22, S160-S160.Biological evaluation and molecular docking studies of AA3052, a compound containing a μ-selective opioid peptide agonist DALDA and D-Phe-Phe-D-Phe-Leu-Leu-NH2, a substance P analogue
Kowalczyk, A.; Kleczkowska, P.; Rekawek, M.; Kulik, K.; Lesniak, A.; Erdei, A.; Borics, A.; Martin, C.; Pawlik, K.; Lipkowski, A. W.; Benyhe, S.; Makulska-Nowak, H.; Ballet, S.; Bujalska-Zadrozny, M., Eur. J. Pharm. Sci 2016, 93, 11-20.Bifunctional Peptide-Based Opioid Agonist Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain.
Guillemyn, K.; Starnowska, J.; Lagard, C.; Dyniewicz, J.; Rojewska, E.; Mika, J.; Chung, N. N.; Utard, V.; Kosson, P.; Lipkowski, A. W.; Chevillard, L.; Arranz-Gibert, P.; Teixido, M.; Megarbane, B.; Tourwe, D.; Simonin, F.; Przewlocka, B.; Schiller, P. W.; Ballet, S., J. Med. Chem.Synthesis of 3-amino-3,4-dihydro-1H-quinolin-2-ones through regioselective palladium-catalyzed intramolecular cyclization.
Halle, F.; Van der Poorten, O.; Doebelin, C.; Niederst, M.; Schneider, S.; Schmitt, M.; Ballet, S.; Bihel, F., Tetrahedron Lett. 2016, 57, 1547-1550.Injectable peptide hydrogels for controlled-release of opioids.
Martin, C.; Oyen, E.; Mangelschots, J.; Bibian, M.; Ben Haddou, T.; Andrade, J.; Gardiner, J.; Van Mele, B.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., MedChemComm 2016, 7, 542-549.Mixed α/β-Peptides as a Class of Short Amphipathic Peptide Hydrogelators with Enhanced Proteolytic Stability.
Mangelschots, J.; Bibian, M.; Gardiner, J.; Waddington, L.; Van Wanseele, Y.; Van Eeckhaut, A.; Acevedo, M. M. D.; Van Mele, B.; Madder, A.; Hoogenboom, R.; Ballet, S., Biomacromolecules 2016, 17, 437-445.Efficient one-pot synthesis of amino-benzotriazolodiazocinone scaffolds via catalyst-free tandem Ugi-Huisgen reactions.
Barlow, T. M. A.; Jida, M.; Guillemyn, A. K.; Tourwe, D.; Caveliers, V.; Ballet, S., Org. Biomol. Chem. 2016, 14, 4669-4677.Synthesis and binding characteristics of [3H]neuromedin N, a NTS2 receptor ligand.
Toth, F.; Mallareddy, J. R.; Tourwe, D.; Lipkowski, A. W.; Bujalska-Zadrozny, M.; Benyhe, S.; Ballet, S.; Toth, G.; Kleczkowska, P., Neuropeptides 2016, 57, 15-20.Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Betti, C.; Starnowska, J.; Mika, J.; Dyniewicz, J.; Frankiewicz, L.; Novoa, A.; Bochynska, M.; Keresztes, A.; Kosson, P.; Makuch, W.; Van Duppen, J.; Chung, N. N.; Broeck, J. V.; Lipkowski, A. W.; Schiller, P.T3P-promoted, mild one-pot syntheses of constrained polycyclic lactam dipeptide analogues via stereoselective Pictet-Spengler and Meyers’ lactamization reactions.
Jida, M.; Van der Poorten, O.; Guillemyn, K.; Urbanczyk-Lipkowska, Z.; Tourwe, D.; Ballet, S., Org. Lett. 2015, 17, 4482-4485.Oxidative alpha,omega-diyne coupling as an approach towards novel peptidic macrocycles.
Verlinden, S.; Geudens, N.; Martins, J. C.; Tourwe, D.; Ballet, S.; Verniest, G., Org. Biomol. Chem. 2015, 13, 9398-9404.Suzuki-Miyaura Diversification of Amino Acids and Dipeptides in Aqueous Media.
Willemse, T.; Van Imp, K.; Goss, R. J. M.; Van Vlijmen, H. W. T.; Schepens, W.; Maes, B. U. W.; Ballet, S., ChemCatChem 2015, 7, 2055-2070.Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist – Neurokinin-1 antagonist peptidomimetics.
Guillemyn, K.; Kleczkowska, P.; Lesniak, A.; Dyniewicz, J.; Van der Poorten, O.; Van den Eynde, I.; Keresztes, A.; Varga, E.; Lai, J.; Porreca, F.; Chung, N. N.; Lemieux, C.; Mika, J.; Rojewska, E.; Makuch, W.; Van Duppen, J.; Przewlocka, B.; Vanden Broeck, J.; Lipkowski, A. W.; Schiller, P.Structural basis for bifunctional peptide recognition at human delta-opioid receptor.
Fenalti, G.; Zatsepin, N. A.; Betti, C.; Giguere, P.; Han, G. W.; Ishchenko, A.; Liu, W.; Guillemyn, K.; Zhang, H.; James, D.; Wang, D.; Weierstall, U.; Spence, J. C. H.; Boutet, S.; Messerschmidt, M.; Williams, G. J.; Gati, C.; Yefanov, O. M.; White, T. A.; Oberthuer, D.; Metz, M.; Yoon, C.Rational design of a hexapeptide hydrogelator for controlled-release drug delivery.
Bibian, M.; Mangelschots, J.; Gardiner, J.; Waddington, L.; Diaz Acevedo, M. M.; De Geest, B. G.; Van Mele, B.; Madder, A.; Hoogenboom, R.; Ballet, S., J. Mater. Chem. B 2015, 3, 759-765.Draft genome sequence analysis of a Pseudomonas putida W15Oct28 strain with antagonistic activity to Gram-positive and Pseudomonas sp. pathogens.
Ye, L. M.; Hildebrand, F.; Dingemans, J.; Ballet, S.; Laus, G.; Matthijs, S.; Berendsen, R.; Cornelis, P., Plos One 2014, 9, e110038Rational Design of Injectable Hexapeptide Hydrogelators for Controlled-Release Drug Delivery.
Bibian, M.; Mangelschots, J.; Martin, C.; Gardiner, J.; Waddington, L.; Acevedo, M. M. D.; Van Mele, B.; Madder, A.; Hoogenboom, R.; Ballet, S., J. Pept. Sci. 2014, 20, S208-S208Efficient synthesis of conformationally constrained, amino-triazoloazepinone-containing di- and tripeptides via a one-pot Ugi-Huisgen tandem reaction.
Barlow, T. M. A.; Jida, M.; Tourwe, D.; Ballet, S., Org. Biomol. Chem. 2014, 12, 6986-6989.One-Pot Isomerization-Cross Metathesis-Reduction (ICMR) Synthesis of Lipophilic Tetrapeptides
Jida, M.; Betti, C.; Schiller, P. W.; Tourwe, D.; Ballet, S., ACS Comb. Sci. 2014, 16, 342-351.Synthesis of Fused 3-Aminoazepinones via Trapping of a new Class of Cyclic Seven-Membered Allenamides with Furan.
Schurgers, B.; Brigou, B.; Urbanczyk-Lipkowska, Z.; Tourwe, D.; Ballet, S.; De Proft, F.; Van Lommen, G.; Verniest, G., Org. Lett. 2014, 16, 3712-3715.Structure revision of N-mercapto-4-formylcarbostyril produced by Pseudomonas fluorescens G308 to 2-(2-hydroxyphenyl)thiazole-4-carbaldehyde [aeruginaldehyde].
Ye, L. M.; Cornelis, P.; Guillemyn, K.; Ballet, S.; Christophersen, C.; Hammerich, O., Nat. Prod. Commun. 2014, 9, 789-794.The First One-Pot Synthesis of l-7-Iodotryptophan from 7-Iodoindole and Serine, and an Improved Synthesis of Other l-7-Halotryptophans.
Smith, D. R. M.; Willemse, T.; Gkotsi, D. S.; Schepens, W.; Maes, B. U. W.; Ballet, S.; Goss, R. J. M., Org. Lett. 2014, 16, 2622-2625.In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt1-DALDA Analogues.
Ballet, S.; Betti, C.; Novoa, A.; Tomboly, C.; Nielsen, C. U.; Helms, H. C.; Lesniak, A.; Kleczkowska, P.; Chung, N. N.; Lipkowski, A. W.; Brodin, B.; Tourwe, D.; Schiller, P. W., ACS Med. Chem. Lett. 2014, 5, 352-357.Hybrid Opioid/Non-Opioid Ligands in Pain Research.
Kleczkowska, P.; W Lipkowski, A.; Tourwe, D.; Ballet, S., Curr. Pharm. Des 2013, 19, 7435-7450.Highly Diastereoselective Synthesis of 1-Carbamoy1-4-aminoindoloazepinone Derivatives via the Ugi Reaction.
Jida, M.; Betti, C.; Urbanczyk-Lipkowska, Z.; Tourwe, D.; Ballet, S., Org. Lett. 2013, 15, 5866-5869.A combinatorial approach to the structure elucidation of a pyoverdine siderophore produced by a Pseudomonas putida isolate and the use of pyoverdine as a taxonomic marker for typing P. putida subspecies.
Ye, L. M.; Ballet, S.; Hildebrand, F.; Laus, G.; Guillemyn, K.; Raes, J.; Matthijs, S.; Martins, J.; Cornelis, P., Biometals 2013, 26, 561-575.Stabilisation of a short α-helical VIP fragment by side chain to side chain cyclisation: a comparison of common cyclisation motifs by circular dichroism.
Frankiewicz, L.; Betti, C.; Guillemyn, K.; Tourwé, D.; Jacquot, Y.; Ballet, S., J. Pept. Sci. 2013, 19, 423-432.Identification of Dmt-D-Lys-Phe-Phe-OH as a highly antinociceptive tetrapeptide metabolite of the opioid-neurotensin hybrid peptide PK20.
Kleczkowska, P.; Bojnik, E.; Leśniak, A.; Kosson, P.; Van den Eynde, I.; Ballet, S.; Benyhe, S.; Tourwé, D.; Lipkowski, A. W., Pharmacological Reports 2013, 65, 836-846.Regulatory mechanisms after short-term and long-term perturbed lysine biosynthesis in the aspartate pathway: the need for isogenes in Arabidopsis thaliana.
Van Bochaute, P.; Novoa, A.; Ballet, S.; Rognes, S. E.; Angenon, G. Physiol. Plant. 2013, 149, 449-460.Amino Triazolo Diazepines (Ata) as Constrained Histidine Mimics.
Buysse, K.; Farard, J.; Nikolaou, A.; Vanderheyden, P.; Vauquelin, G.; Pedersen, D. S.; Tourwe, D.; Ballet, S., Org. Lett. 2011, 13, 6468-6471.Variation of the Net Charge, Lipophilicity, and Side Chain Flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Novoa, A.; Van Dorpe, S.; Wynendaele, E.; Spetea, M.; Bracke, N.; Stalmans, S.; Betti, C.; Chung, N. N.; Lemieux, C.; Zuegg, J.; Cooper, M. A.; Tourwé, D.; De Spiegeleer, B.; Schiller, P. W.; Ballet, S., J. Med. Chem. 2012, 55, 9549-9561.In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist - neurokinin 1 receptor antagonist chimera.
Guillemyn, K.; Kleczkowska, P.; Novoa, A.; Vandormael, B.; Van den Eynde, I.; Kosson, P.; Asim, M. F.; Schiller, P. W.; Spetea, M.; Lipkowski, A. W.; Tourwé, D.; Ballet, S., Molecular Brain 2012, 5, 4-4.Asymmetric Synthesis and Conformational Analysis by NMR Spectroscopy and MD of Aba- and alpha-MeAba-Containing Dermorphin Analogues.
Vandormael, B.; De Wachter, R.; Martins, J. C.; Hendrickx, P. M. S.; Keresztes, A.; Ballet, S.; Mallareddy, J. R.; Toth, F.; Toth, G.; Tourwe, D., ChemMedChem 2011, 6, 2035-2047.Synthesis, Biological Evaluation, and Automated Docking of Constrained Analogues of the Opioid Peptide H-Dmt-D-Ala-Phe-Gly-NH2 Using the 4- or 5-Methyl Substituted 4-Amino-1,2,4,5-tetrahydro-2-benzazepin-3-one Scaffold
De Wachter, R.; de Graaf, C.; Keresztes, A.; Vandormael, B.; Ballet, S.; Toth, G.; Rognan, D.; Tourwe, D., J. Med. Chem. 2011, 54, 6538-6547.Design of Novel Neurokinin 1 Receptor Antagonists Based on Conformationally Constrained Aromatic Amino Acids and Discovery of a Potent Chimeric Opioid Agonist-Neurokinin 1 Receptor Antagonist.
Ballet, S.; Feytens, D.; Buysse, K.; Chung, N. N.; Lemieux, C.; Tumati, S.; Keresztes, A.; Van Duppen, J.; Lai, J.; Varga, E., J. Med. Chem. 2011, 54, 2467-2476.PK20, a new opioid-neurotensin hybrid peptide that exhibits central and peripheral antinociceptive effects.
Kleczkowska, P.; Kosson, P.; Ballet, S.; Van den Eynde, I.; Tsuda, Y.; Tourwé, D.; Lipkowski, A. W., Mol Pain 2010, 6, 86-92.Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Ballet, S.; Marczak, E. D.; Feytens, D.; Salvadori, S.; Sasaki, Y.; Abell, A. D.; Lazarus, L. H.; Balboni, G.; Tourwé, D., Bioorg. Med. Chem. Lett. 2010, 20, 1610-1613.Synthesis and High-Resolution NMR Structure of a beta(3)-Octapeptide with and without a Tether Introduced by Olefin Metathesis.
Ebert, M. O.; Gardiner, J.; Ballet, S.; Abell, A. D.; Seebach, D., Helv. Chim. Acta 2009, 92, 2643-2658.Conformationally constrained opioid ligands: The Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Ballet, S.; Feytens, D.; De Wachter, R.; De Vlaeminck, M.; Marczak, E. D.; Salvadori, S.; de Graaf, C.; Rognan, D.; Negri, L.; Lattanzi, R.; Lazarus, L. H.; Tourwe, D.; Balboni, G., Bioorg. Med. Chem. Lett. 2009, 19, 433-437.Influence of ring substitution on the conformation and beta-turn mimicry of 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one peptide mimetics.
De Wachter, R.; Brans, L.; Ballet, S.; Van den Eynde, I.; Feytens, D.; Keresztes, A.; Toth, G.; Urbanczyk-Lipkowska, Z.; Tourwe, D., Tetrahedron 2009, 65, 2266-2278.Cross-metathesis and ring-closing metathesis reactions of amino acid-based substrates.
Vernall, A. J.; Ballet, S.; Abell, A. D., Tetrahedron 2008, 64, 3980-3997.Blood-Brain barrier penetration by two dermorphin tetrapeptide analogues: Role of lipophilicity vs structural flexibility.
Ballet, S.; Misicka, A.; Kosson, P.; Lemieux, C.; Chung, N. N.; Schiller, P. W.; Lipkowski, A. W.; Tourwe, D., J. Med. Chem. 2008, 51, 2571-2574.Endomorphin-2 with a beta turn backbone constraint retains the potent mu-opioid receptor agonist properties.
Tomboly, C.; Ballet, S.; Feytens, D.; Kover, K. E.; Borics, A.; Lovas, S.; Al-Khrasani, M.; Furst, Z.; Toth, G.; Benyhe, S.; Tourwe, D., J. Med. Chem. 2008, 51, 173-177.Multiple Ligands in Opioid Research.
Ballet, S.; Pietsch, M.; Abell, A. D., Protein Pep. Lett. 2008, 15, 668-682.High-performance liquid chromatographic separation of stereoisomers of N-phthaloyl-protected amino acids and dipeptidomimetics.
Illisz, I.; Ballet, S.; Van Rompaey, K.; De Wachter, R.; Tourwe, D.; Armstrong, D. W.; Peter, A., J. Sep. Sci. 2007, 30, 1881-1887.Novel Selective human melanocortin-3 receptor ligands : Use of the 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffold.
Ballet, S.; Mayorov, A. V.; Cai, M. Y.; Tymecka, D.; Chandler, K. B.; Palmer, E. S.; Van Rompaey, K.; Misicka, A.; Tourwe, D.; Hruby, V. J., Bioorg. Med. Chem. Lett. 2007, 17, 2492-2498.Derivatization of 1-phenyl substituted 4-amino-2benzazepin-3-ones : evaluation of Pd-catalyzed coupling reactions.
Ballet, S.; De Wachter, R.; Maes, B. U. W.; Tourwe, D., Tetrahedron 2007, 63, 3718-3727.Bradykinin analogs containing the 4-amino-2-benzazepin-3-one scaffold at the C-terminus.
Ballet, S.; De Wachter, R.; Van Rompaey, K.; Tömböly, C.; Feytens, D.; Töth, G.; Quartara, L.; Cucchi, P.; Meini, S.; Tourwé, D., J. Pept. Sci. 2007, 13, 164-170.beta-Methyl substitution of cyclohexylalanine in Dmt-Tic-Cha-Phe peptides results in highly potent delta opioid antagonists.
Toth, G.; Ioja, E.; Tomboly, C.; Ballet, S.; Tourwe, D.; Peter, A.; Martinek, T.; Chung, N. N.; Schiller, P. W.; Benyhe, S.; Borsodi, A., J. Med. Chem. 2007, 50, 328-333.Synthesis and evaluation of the beta-turn properties of 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-ones and of their spirocyclic derivative.
Van Rompaey, K.; Ballet, S.; Tomboly, C.; De Wachter, R.; Vanommeslaeghe, K.; Biesemans, M.; Willem, R.; Tourwe, D., Eur. J. Org. Chem. 2006, 2899-2911.New 2',6'-dimethyl-L-Tyrosine (Dmt) Opioid Peptidomimetics Based on the Aba-Gly Scaffold. Development of Unique µ-Opioid Receptor Ligands.
Ballet, S.; Salvadori, S.; Trapella, C.; Bryant, S. D.; Jinsmaa, Y.; Lazarus, L. H.; Negri, L.; Giannini, E.; Lattanzi, R.; Tourwe, D.; Balboni, G., J. Med. Chem. 2006, 49, 3990-3993.Synthesis of substituted 4-amino-2-benzezepin-3-ones via N-acyliminium ion cycliations.
Ballet, S.; Urbanczyk-Lipkowska, Z.; Tourwe, D., Synlett 2005, 2791-2795.Synthesis of 4-amino-1,2,4,5-tetrahydro-2-benzazepine-3-ones and study of their beta-turn inducing properties.
Van den Eynde, I.; Van Rompaey, K.; Ballet, S.; De Wachter, R.; Van Ommeslaeghe, K.; Biesemans, M.; Willem, R.; Tourwe, D., Biopolymers 2005, 80, 569-569.Synthesis and biological evaluation of constrained analogues of the opioid peptide H-Tyr-D-Ala-Phe-Gly-NH2 using 4-amino-2-benzazepin-3-one scaffold.
Ballet, S.; Frycia, A.; Piron, J.; Chung, N.; Schiller, P. W.; Kosson, P.; Lipkowski, A.; Tourwe, D., J. Pept. Res. 2005, 66, 222-230.
Prof. Ulrich Hennecke
Paracoccus kondratievae produces poly(3-hydroxybutyrate) under elevated temperature conditions
R. Moanis, H. Geeraert, N. Van den Brande, U. Hennecke, E, Peeters, Environ. Microbiol. Rep. 2024, 16, e13260.Fast Self-Assembly Dynamics of a β-Sheet Peptide Soft Material
J. Bertouille, S. Kasas, C. Martin, U. Hennecke, S. Ballet, R. Willaert, R. G., Small, 2023, 2206795.Azetidomonamide and diazetidomonapyridone metabolites control biofilm formation and pigment synthesis in Pseudomonas aeruginosa
S. Ernst, A. Volkov, M. Stark, L. Hölscher, K. Steinert, S. Fetzner, U. Hennecke, S. L. Drees, J. Am. Chem. Soc. 2022, 144, 7676-7685.Brønsted Acid-Catalysed Enantioselective Iodocycloetherification Enabled by Triphenylphosphine Selenide Cocatalysis
S. Guria, C. G. Daniliuc, U. Hennecke, Adv. Synth. Catal. 2021, 363, 3852-3858.A dynamic picture of the halolactonization reaction through a combination of ab initio metadynamics and experimental investigations
R. Van Lommel, J. Bock, C.G. Daniliuc, U. Hennecke, F. De Proft, Chem. Sci. 2021, DOI: 10.1039/D1SC01014J.Modification of the Pseudomonas aeruginosa toxin 2-heptyl-1-hydroxyquinolin-4(1H)-one and other secondary metabolites by methyltransferases from mycobacteria
P. Sartor, J. Bock, U. Hennecke, S. Thierbach, S. Fetzner, FEBS J. 2021, 288, 2360-2376.Enantioselective Dihalogenation of Alkenes
U. Hennecke, J. Bock, S. Guria, V. Wedek, Chem. Eur. J. 2021, 27, 4517-4530.Enantioselective Dihalogenation of Alkenes
J. Bock, S. Guria, V. Wedek, U. Hennecke, Chem. Eur. J. 2021, 27, 4517-4530.Structural basis for recognition and ring-cleavage of the Pseudomonas quinolone signal (PQS) by AqdC, a mycobacterial dioxygenase of the α/β-hydrolase fold family
S. C. Wullich, S. Kobus, M. Wienhold, U. Hennecke, S. H. J. Smits, S. Fetzner, J. Struc. Biol. 2019, 207, 287-294.Bromination of alkyl quinolones by Microbulbifer sp. HZ11, a marine Gammaproteobacterium, modulates their antibacterial activity
N. H. Ritzmann, A. Mährlein, S. Ernst, U. Hennecke, S. L. Drees, S. Fetzner, Environ. Microbiol. 2019, 21, 2595-2609.Organocatalytic, Enantioselective Dichlorination of Unfunctionalized Alkenes
V. Wedek, R. Van Lommel, C. G. Daniliuc, F. De Proft, U. Hennecke, Angew. Chem. Int. Ed. 2019, 58, 9239-9243.Stable Bromiranium Ion Salts as Reagents for Biomimetic Indole Terpenoid Cyclizations
J. Bock, C. G. Daniliuc, U. Hennecke, Org. Lett. 2019, 21, 1704-1707.Synthesis, structural characterisation, and synthetic application of stable seleniranium ions
J. Bock, C. G. Daniliuc, K. Bergander, C. Mück-Lichtenfeld, U. Hennecke, Org. Biomol. Chem. 2019, 17, 3181-3185.Synthesis and biological activity of methylated derivatives of the Pseudomonas metabolites HHQ, HQNO and PQS
S. Thierbach, M. Wienhold, S. Fetzner, U. Hennecke, Beilstein J. Org. Chem. 2019, 15, 187-193.PqsL uses reduced flavin to produce 2-hydroxylaminobenzoylacetate, a preferred PqsBC substrate in alkyl quinolone biosynthesis in Pseudomonas aeruginosa
S. L. Drees, S. Ernst, B. Belviso, N. Jagmann, U. Hennecke, S. Fetzner, J. Biol. Chem. 2018, 293, 9345-9357.An Enantioselective Iodolactonization/Cross-Coupling Protocol for the Synthesis of Highly-Substituted Enol Lactones
C. Fricke, M. Wilking, C. G. Daniliuc, U. Hennecke, Eur. J. Org. Chem. 2018, 3158-3166.Chemical Modification and Detoxification of the Pseudomonas aeruginosa Toxin 2-Heptyl-4-hydroxyquinoline N-Oxide by Environmental and Pathogenic Bacteria
S. Thierbach, F. S. Birmes, M. C. Letzel, U. Hennecke, S. Fetzner, ACS Chem. Biol. 2017, 12, 2305-2312.Stable Bromiranium Ions with Weakly-Coordinating Counterions as Efficient Electrophilic Brominating Agents
C. Ascheberg, J. Bock, F. Buß, C. Mück-Lichtenfeld, C. G. Daniliuc, K. Bergander, F. Dielmann, U. Hennecke, Chem. Eur. J. 2017, 23, 11578-11586.Why DNA is a More Effective Scaffold than RNA in Nucleic Acid-based Asymmetric Catalysis – Supramolecular Control of Cooperative Effects
J. J. Marek, U. Hennecke, Chem. Eur. J. 2017, 23, 6009-6013.Enantioselective Catalysis using short, structurally-defined DNA Hairpins as Scaffold for Hybrid Catalysts
J. J. Marek, R. Singh, A. Heuer, U. Hennecke, Chem. Eur. J. 2017, 23, 6004-6008.Synthesis of Chiral Heterocyclic N-Haloamides and -imides and their Application as Halogenating Agents and Mechanistic Probes
U. Hennecke, C. H. Müller, C. G. Daniliuc, Eur. J. Org. Chem. 2017, 484-490.Monomeric cinchona alkaloid-based catalysts for highly enantioselective bromolactonisation of alkynes
M. Wilking, C. G. Daniliuc, U. Hennecke, Chem. Eur. J. 2016, 51, 18601-18607.PqsBC, a condensing enzyme in the biosynthesis of the Pseudomonas aeruginosa quinolone signal: crystal structure, inhibition, and reaction mechanism
S. L. Drees, C. Li, F. Prasetya, M. Saleem, I. Dreveny, P. Williams, U. Hennecke, J. Emsley, S. Fetzner, J. Biol. Chem. 2016, 291, 6610-6624.1-Iodo-n-Heteroatom-Functionalized Alkanes (n ≥ 2 with Both Functions Formed Simultaneously: Synthesis by Addition across C=C Bond
U. Hennecke in Science of Synthesis Knowledge Updates 2015/2, T. Wirth (Ed.), Thieme, Stuttgart, 2015, 449-465.Homohalocyclization: Electrophilic Bromine-Induced Cyclizations of Cyclopropanes
C. Rösner, U. Hennecke, Org. Lett. 2015, 17, 3226-3229.Iodoalkanes: Synthesis by Addition to π-Type C-C-Bonds (Update 2014)
U. Hennecke in Science of Synthesis Knowledge Updates 2015/2, T. Wirth (Ed.), Thieme, Stuttgart, 2015, 437-448.Asymmetric, Organocatalytic Bromolactonization of Allenoic Acids
M. Wilking, C. G. Daniliuc, U. Hennecke, Synlett 2014, 25, 1701-1704.Enantioselective Haloetherifications Catalyzed by 1,1’-Bi-2-naphthol (BINOL) Phosphates: From Symmetrical Alkenediols to Simple Alkenols
C. H. Müller, C. Rösner, U. Hennecke, Chem. Asian J. 2014, 9, 2162-2169.Desymmetrization as a Strategy in Asymmetric Halocyclization Reactions
M. Wilking, U. Hennecke, Synlett 2014, 25, 1633-1637.Addition Reactions with Formation of Carbon–Halogen Bonds
U. Hennecke, T. Wald, C. Rösner, T. Robert, M. Oestreich, in Comprehensive Organic Synthesis 2nd Edition, G. A. Molander, P. Knochel (Eds.), Elsevier, Oxford, 2014, Vol. 7 (Oxidation), 638-691.The Influence of G-Quadruplex Structure on DNA-based Asymmetric Catalysis Using the G-Guadruplex-Bound Cationic Porphyrin TMPyP4·Cu
M. Wilking, U. Hennecke, Org. Biomol. Chem. 2013, 11, 6940-6945.Enantioselective, Desymmetrizing Bromolactonization of Alkynes
M. Wilking, C. Mück-Lichtenfeld, C. G. Daniliuc, U. Hennecke, J. Am. Chem. Soc. 2013, 135, 8133-8136.Efficient Synthesis of Chiral 2,2’-Bipyrrolidines by an anti-Selective Alkene Diamination
C H. Müller, R. Fröhlich, C. G. Daniliuc, U. Hennecke, Org. Lett. 2012, 14, 5944-5947.A New Approach towards the Asymmetric Fluorination of Alkenes Using Anionic Phase-Transfer Catalysts
U. Hennecke, Angew. Chem. Int. Ed. 2012, 51, 4532-4534.Hydrolase-Like Properties of a Cofactor-Independent Dioxygenase
S. Thierbach, K. Büldt-Karentzopoulos, A. Dreiling, U. Hennecke, S. König, S. Fetzner, ChemBioChem 2012, 13, 1125-1127.New Catalytic Approaches towards the Enantioselective Halogenation of Alkenes
U. Hennecke, Chem. Asian J. 2012, 7, 456-465.Catalytic, Asymmetric, Bromine-induced Semipinacol Rearrangements at Unactivated Double Bonds
C. H. Müller, M. Wilking, A. Rühlmann, B. Wibbeling, U. Hennecke, Synlett 2011, 2043-2047.Enantioselective Haloetherification by Asymmetric Opening of meso-Halonium Ions
U. Hennecke, C. H. Müller, R. Fröhlich, Org. Lett. 2011, 13, 860-863.Sequential Double α-Arylation of N-Allylureas by Asymmetric Deprotonation and N→C Aryl Migration
D. J. Tetlow, U. Hennecke, J. Raftery, M. J. Waring, D. S. Clarke, J. Clayden, Org. Lett. 2010, 12, 5442-5445.The Origin of the Conformational Preference of N,N'-diaryl-N,N'-dimethyl ureas
J. Clayden, U. Hennecke, M. A. Vincent, I. H. Hillier, M. Helliwell, Phys. Chem. Chem. Phys. 2010, 12, 15056-15064.Crystal Structure of the T(6-4)C Lesion in Complex with a (6-4) DNA Photolyase and Repair of UV-Induced (6-4) and Dewar Photolesions
A. F. Glas, S. Schneider, M. J. Maul, U. Hennecke, T. Carell, Chem. Eur. J. 2009, 15, 10387-10396.N to C Aryl Migration in Lithiated Carbamates: alpha-Arylation of Benzylic Alcohols
J. Clayden, W. Farnaby, D. M. Grainger, U. Hennecke, M. Mancinelli, D. J. Tetlow, I. H. Hillier, M. A. Vincent, J. Am. Chem. Soc. 2009, 131, 3410-3411.α-Arylation of Cyclic Amines by Aryl Transfer in Lithiated Ureas
R. Bach, J. Clayden, U. Hennecke, Synlett 2009, 421-424.Recognition and Repair of UV Lesions in Loop Structures of Duplex DNA by DASH-Type Cryptochrome
R. Pokorny, T. Klar, U. Hennecke, T. Carell, A. Batschauer, L.-O. Essen, Proc. Natl. Acad. Sci. U. S. A. 2008, 105, 21023-21027.α-Pyridinylation of Chiral Amines via Urea Coupling, Lithiation and Rearrangement: Synthesis of α-Arylated Nicotine Analogues
J. Clayden, U. Hennecke, Org. Lett. 2008, 10, 3567-3570.A General Route to 4-C-Substituted Pyrimidine Nucleosides
U. Hennecke, D. Kuch, T. Carell, Synthesis 2007, 929-935.CPD Damage Recognition by Transcribing RNA Polymerase II
F. Brückner, U. Hennecke, T. Carell, P. Cramer, Science 2007, 315, 859-862.Characterization of a New Thermophilic Spore Photoproduct Lyase from Geobacillus stearothermophilus (SplG) with Defined Lesion Containing DNA Substrates
J. C. Pieck, U. Hennecke, A. J. Pierik, M. G. Friedel, T. Carell, J. Biol. Chem. 2006, 281, 36317-36326.Natural and Non-Natural Antenna Chromophores in the DNA Photolyase from Thermus Thermophilus
T. Klar, G. Kaiser, U. Hennecke, T. Carell, A. Batschauer, L.-O. Essen, ChemBioChem 2006, 7, 1798-1806.Investigation of the Pathways of Excess Electron Transfer in DNA with Flavin-Donor and Oxetane-Acceptor Modified DNA Hairpins
S. Breeger, M. von Meltzer, U. Hennecke, T. Carell, Chem. Eur. J. 2006, 12, 6469-6477.Crystal Structure of a Photolyase Bound to a CPD-Like DNA Lesion after in situ Repair
A. Mees, T. Klar, P. Gnau, U. Hennecke, A. P. M. Eker, T. Carell, L.-O. Essen, Science 2004, 306, 1789-1793.Excess Electron Transfer in Defined Donor-Nucleobase and Donor-DNA-Acceptor Systems
C. Behrens, M. K. Cichon, F. Grolle, U. Hennecke, T. Carell, Top. Curr. Chem. 2004, 236, 187-204.Excess Electron Transport through DNA: a Single Electron Repairs More Than One UV-Induced Lesion
B. Giese, B. Carl, T. Carl, T. Carell, C. Behrens, U. Hennecke, O. Schiemann, E. Feresin, Angew. Chem. Int. Ed. 2004, 43, 1848-1851.Excess Electron-Transfer-based Repair of a cis-syn Thymine Dimer in DNA is not Sequence Dependent
S. Breeger, U. Hennecke, T. Carell, J. Am Chem. Soc. 2004, 126, 1302-1303.Design of Luminescent Polymers for LEDs
A. B. Holmes, A. D. Bond, J. E. Davies, C. Fischmeister, J. Frey, U. Hennecke, J. Li, Y. Ma, R. E. Martin, I. D. Rees, K. Robinson, T. Sano, F. Cacialli, S. F. Lim, R. H. Friend, Mater. Res. Soc. Symp. Proc. 2002, 708, 185-195.New Family of Polyfluorene Copolymers for Light Emitting Devices
A. B. Holmes, I. Rees, T. Sano, C. Fischmeister, J. Frey, U. Hennecke, C.-S. Tuan, B. S. Chuah, Y. Ma, R. E. Martin, J. Li, N. Feeder, A. Bond, F. Cacialli, S. Lim, R. Friend, Proceedings of SPIE-The International Society for Optical Engineering 2002, 4464, 42-48.
Prof. Charlotte Martin
Fluorinated Peptide Hydrogels Result in Longer In Vivo Residence Time after Subcutaneous Administration
Honfroy, A., Bertouille, J., Turea, A., Cauwenbergh, T., Bridoux, J., Lensen, M., Mangialetto, J., Van den Brande, N., White, J., Gardiner, J., Brigaud, T., Ballet, S., Hernot, S., Chaume, G., Martin, D., DOI: 10.1021/acs.biomac.4c00872Multitarget µ-opioid receptor agonists-neuropeptide FF receptor antagonists induce potent antinociception with reduced adverse side effects.
De Neve, J.; Elhabazi, K.§; Gonzalez, S.; Herby, C.; Schneider, S.; Utard, V.; Fellmann-Clauss, R.; Petit-Demouliere, N.; Lecat, S.; Kremer, M.; Ces, A.; Daubeuf, F.; Martin, C.; Ballet, S.; Bihel, F.; Simonin, F., J Med Chem. 2024 May 9;67(9):7603-7619.Peptide Sequence Variations Govern Hydrogel Stiffness: Insights from a Multi-Scale Structural Analysis of H-FQFQFK-NH2 Peptide Derivatives
T. De Maeseneer, T. Cauwenbergh, J. Gardiner, J. F. White, W. Thielemans, C. Martin, P. Moldenaers, S. Ballet, R. Cardinaels, Macromol Biosci. 2024 Mar 29:e2300579.Structure-Based Design and Synthesis of Stapled 10Panx1 Analogues for Use in Cardiovascular Inflammatory Diseases
Lamouroux, A.; Tournier, M.; Iaculli, D.; Caufriez, A.; Rusiecka, O.M.; Martin, C.; Bes, V.; Carpio, L.E.; Girardin, Y.; Loris, R.; Tabernilla, A.; Molica, F.; Gozalbes, R.; Mayán, M.D.; Vinken, M.; Kwak, B.R.; Ballet, S.; J. Med. Chem. 2023, 66, 18, 13086–13102Identification of small molecule antivirals against HTLV-1 by targeting the hDLG1-Tax-1 protein-protein interaction
Maseko, S.B.; Brammerloo, Y.; Van Molle, I.; Sogues, A.; Martin, C.; Gorgulla, C.; Plant, E.; Olivet, J.; Blavier, J.; Ntombela, T.; Delvigne, F.; Arthanari, H.; El Hajj, H.; Bazarbachi, A.; Van Lint, C.; Salehi-Ashtiani, K.; Remaut, H.; Ballet, S.; Volkov, A.N.; Twizere, J-C.; Antiviral Research, 2Bypassing the Need for Cell Permeabilization: Nanobody CDR3 Peptide Improves Binding on Living Bacteria
Breine, A.; Van holsbeeck, K.; Martin, C.; Gonzalez, S.; Mannes, M.; Pardon, E.; Steyaert, J.; Remaut, H.; Ballet, S.; Van der Henst, C.; Bioconjugate Chem. 2023, 34, 7, 1234-1243Determination of structural features that underpin the pannexin1 channel inhibitory activity of the peptide 10Panx1
Caufriez, A.; Lamouroux, A.; Martin, C.; Iaculli, D.; Ergüç, EI.; Gozalbes, R.; Mayan, M.D.; Kwak, B.R.; Tabernilla, A.; Vinken, M.; Ballet, S., Bioorg. Chem. 2023 DOI: 10.1016/j.bioorg.2023.106612Nanobody Loop Mimetics Enhance Son of Sevenless 1-Catalyzed Nucleotide Exchange on RAS
Van holsbeeck, K., Fischer, B., Gonzalez, S., Gadais, C., Versées, W., Martins, J. C., Martin, C., Wohlkönig, A., Steyaert, J., Ballet, S., Angew. Chem. Int. Ed. 2023, e202219095; Angew. Chem. 2023, e202219095.Fast Self-Assembly Dynamics of a β-Sheet Peptide Soft Material
J. Bertouille, S. Kasas, C. Martin, U. Hennecke, S. Ballet, R. Willaert, R. G., Small, 2023, 2206795.Bifunctional Peptidomimetic G Protein-Biased Mu-Opioid Receptor Agonist and Neuropeptide FF Receptor Antagonist KGFF09 Shows Efficacy in Visceral Pain without Rewarding Effects after Subcutaneous Administration in Mice
There is still an unmet clinical need to develop new pharmaceuticals for effective and safe pain management. Current pharmacotherapy offers unsatisfactory solutions due to serious side effects related to the chronic use of opioid drugs.Impact of doubling peptide length on in vivo hydrogel stability and sustained drug release
Heremans, J.; Chevillard, L.; Mannes, M.; Mangialetto, J.; Leroy, K; White, J.F.; Lamouroux, A.; Vinken, M.; Gardiner, J.; Van Mele, B.; Van den Brande, N.; Hoogenboom, R.; Madder, A.; Caveliers, V.; Mégarbane ,B.; Hernot, S.; Ballet, S.; Martin, C., Journal of Controlled Release, 2022,350, 514-524Harnessing the anti-nociceptive potential of NK2 and NK3 ligands in the design of new multifunctional µ/δ-opioid agonist-neurokinin antagonist peptidomimetics.
Gadais, C.; Piekielna-Ciesielska, J.; De Neve, J.; Martin, C.; Janecka, A.; Ballet, S.Towards the understanding of halogenation in peptide hydrogels: a quantum chemical approach.
Bettens, T.; Lacanau, V.; Van Lommel, R.; De Maeseneer, T.; Vandeplassche, W.; Brancart, J.; Barlow, T.; Woller, T. M.; Van den Brande, N.; Moldenaers, P.; De Proft, F.; Madder, A.; Hoogenboom, R.; Martin, C.; Ballet, S.; Alonso Giner, M. Materials Advances, 2021 2(14), 4792-4803.Development of Generic G Protein Peptidomimetics Able to Stabilize Active State Gs Protein‐Coupled Receptors for Application in Drug Discovery
Mannes, M.; Martin, C.; Triest, S.; Pia Dimmito, M.; Mollica, A.; Laeremans, T.; Menet, C.J.; Ballet, S., Angew. Chem. Int. Ed. 2021. https://doi.org/10.1002/anie.202100180Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure
Martin, C.; Gimenez, L. E.; Williams, S. Y.; Jing, Y.; Wu, Y.; Hollanders, C.; Van der Poorten, O.; Gonzalez, S.; Van holsbeeck, K.; Previti, S.; Lamouroux, A.; Zhao, S.; Tourwé, D.; Stevens R.C.; Cone R.D.; Ballet, S., J. Med. Chem. 2021, 64, 1, 357–369Anti-human PD-L1 Nanobody for Immuno-PET Imaging: Validation of a Conjugation Strategy for Clinical Translation
Bridoux, J.; Broos, K.; Lecocq, Q.; Debie, P.; Martin, C.; Ballet, S.; Raes, G.; Neyt, S.; Vanhove, C.; Breckpot, K.; Devoogdt, N.; Caveliers, V.; Keyaerts, M.; Xavier, C.; Biomolecules, 2020, 10(10), 1388.Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies
Gonzalez, S.; Dumitrascuta, M.; Eiselt, E.; Louis, S.; Kunze, L.; Blasiol, A.; Vivancos, M.; Previti,S.; Dewolf, E.; Martin, C.; Tourwé, D.; Cavelier, F.; Gendron, L.; Sarret, P.; Spetea, M.; Ballet, S.; J. Med. Chem. 2020, 63, 21, 12929–12941Peptide-based targeting of connexins and pannexins for therapeutic purposes
Caufriez, A;, Böck, D.; Martin, C.; Ballet, S.; Vinken, M.; Expert Opinion on Drug Discovery, 2020, 15(10), 1213-1222.A New Family of Diverse Skin Peptides from the Microhylid Frog Genus Phrynomantis
Raaymakers, C.; Stijlemans, B.; Martin, C.; Zaman, S.; Ballet, S.; Martel, A.; Pasmans, F.; Roelants, K. Molecules 2020, 25(4), 912Zn-Catalyzed Nicotinate-Directed Transamidations in Peptide Synthesis
Hollanders, C.; Renders, E.; Gadais, C.; Masullo, D.; Van Raemdonck, L.; Wybon, C. C. D.; Martin, C.; Herrebout, W. A.; Maes, B. U. W.; Ballet, S. ACS Catal., 2020 DOI: 10.1021/acscatal.9b05074Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists.
Claff, T.; Yu, J.; Blais, V.; Patel, N.; Martin, C.; Wu, L.; Han, G. W.; Holleran, B. J.; Van der Poorten, O.; White, K. L.; Hanson, M. A.; Sarret, P.; Gendron, L.; Cherezov, V.; Katritch, V.; Ballet, S.; Liu, Z.-J.; Müller, C. E.; Stevens, R. C., Sci. Adv 2019, 5, eaax9115.Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia.
Eiselt, E.; Gonzalez, S.; Martin, C.; Chartier, M.; Betti, C.; Longpré, J.-M.; Cavelier, F.; Tourwé, D.; Gendron, L.; Ballet, S.; Sarret, P., ACS Chem. Neurosci. 2019, 10, 4535-4544.Trifluoromethylated Proline Surrogates as Part of “Pro–Pro” Turn-Inducing Templates.
Gadais, C.; Van holsbeeck, K.; Moors, S. L. C.; Buyst, D.; Fehér, K.; Van Hecke, K.; Tourwé, D.; Brigaud, T.; Martin, C.; De Proft, F.; Pytkowicz, J.; Martins, J. C.; Chaume, G.; Ballet, S., ChemBioChem 2019, 20, 2513-2518.Radiometal-labeled anti-VCAM-1 nanobodies as molecular tracers for atherosclerosis – impact of radiochemistry on pharmacokinetics.
Bala, G.; Crauwels, M.; Blykers, A.; Remory, I.; Marschall Andrea, L. J.; Dübel, S.; Dumas, L.; Broisat, A.; Martin, C.; Ballet, S.; Cosyns, B.; Caveliers, V.; Devoogdt, N.; Xavier, C.; Hernot, S., Biol. Chem., 2019; 400, 323.Modulating peptide hydrogel strength through halogenation.
Vandeplassche, W.; Ballet, S.; Martin, C.; Hoogenboom, R.; Madder, A., J. Pept. Sci. 2018, 24, S109-S110.Design, synthesis and biological evaluation of stapled helical peptides targeting the myddosome.
Terriers, V.; Verhoeven, J.; Martin, C.; Hollanders, K.; Triballeau, N.; Mollat, P.; Van der Plas, S.; De Wilde, G.; Ballet, S., J. Pept. Sci. 2018, 24, S157-S157.A Bifunctional Biased Mu Opioid Agonist - Neuropeptide FF Receptor Antagonist as Analgesic with Improved Acute and Chronic Side Effects.
la Rochelle, A. D.; Guillemyn, K.; Dumitrascuta, M.; Gonzalez, S.; Martin, C.; Utard, V.; Quillet, R.; Schneider, S.; Daubeuf, F.; Willemse, T.; Mampuys, P.; Maes, B.; Frossard, N.; Bihel, F.; Spetea, M.; Simonin, F.; Ballet, S., J. Pept. Sci. 2018, 24, S156-S156.Trifluoromethylated proline surrogates as part of 'Pro-Pro' turn-inducing templates for the design of beta-hairpin mimetics.
Gadais, C.; Van Holsbeeck, K.; Moors, S.; Feher, K.; Pytkowicz, J.; Martins, J.; De Proft, F.; Tourwe, D.; Brigaud, T.; Martin, C.; Chaume, G.; Ballet, S., J. Pept. Sci. 2018, 24, S117-S117.Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.
Martin, C.; Dumitrascuta, M.; Mannes, M.; Lantero, A.; Bucher, D.; Walker, K.; Van Wanseele, Y.; Oyen, E.; Hernot, S.; Van Eeckhaut, A.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., J. Med. Chem. 2018, 61, 9784-9789.A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects.
la Rochelle, A. D.; Guillemyn, K.; Dumitrascuta, M.; Martin, C.; Utard, V.; Quillet, R.; Schneider, S.; Daubeuf, F.; Willemse, T.; Mampuys, P.; Maes, B. U. W.; Frossard, N.; Bihel, F.; Spetea, M.; Simonin, F.; Ballet, S., Pain 2018, 159, 1705-1718.Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists.
De Prins, A.; Martin, C.; Van Wanseele, Y.; Tomboly, C.; Tourwe, D.; Caveliers, V.; Holst, B.; Van Eeckhaut, A.; Rosenkilde, M. M.; Smolders, I.; Ballet, S., ACS Med. Chem. Lett 2018, 9, 496-501.Development of potent and proteolytically stable human neuromedin U receptor agonists.
De Prins, A.; Martin, C.; Van Wanseele, Y.; Skov, L. J.; Tomboly, C.; Tourwe, D.; Caveliers, V.; Van Eeckhaut, A.; Holst, B.; Rosenkilde, M. M.; Smolders, I.; Ballet, S., Eur. J. Med. Chem. 2018, 144, 887-897.Rational Design of Nanobody80 Loop Peptidomimetics: Towards Biased beta(2) Adrenergic Receptor Ligands.
Martin, C.; Moors, S. L. C.; Danielsen, M.; Betti, C.; Fabris, C.; Pedersen, D. S.; Pardon, E.; Peyressatre, M.; Feher, K.; Martins, J. C.; Mathiesen, J. M.; Morris, M. C.; Devoogdt, N.; Caveliers, V.; De Proft, F.; Steyaert, J.; Ballet, S., Eur. Chem. J. 2017, 23, 9632-9640.The antibacterial prodrug activator Rv2466c is a mycothiol-dependent reductase in the oxidative stress response of Mycobacterium tuberculosis.
Rosado, L. A.; Wahni, K.; Degiacomi, G.; Pedre, B.; Young, D.; de la Rubia, A. G.; Boldrin, F.; Martens, E.; Marcos-Pascual, L.; Sancho-Vaello, E.; Albesa-Jove, D.; Provvedi, R.; Martin, C.; Makarov, V.; Versees, W.; Verniest, G.; Guerin, M. E.; Mateos, L. M.; Manganelli, R.; Messens, J., J. Biol.In Vivo Imaging of the Stability and Sustained Cargo Release of an Injectable Amphipathic Peptide-Based Hydrogel.
Oyen, E.; Martin, C.; Caveliers, V.; Madder, A.; Van Mele, B.; Hoogenboom, R.; Hemot, S.; Ballet, S., Biomacromolecules 2017, 18, 994-1001.