Publications

Prof. Steven Ballet

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/ph15080935

Wandering beyond small molecules: peptides as allosteric protein modulators

Mannes, M.; Martin, C.; Menet, C.; Ballet, S. Trends Pharmacol. Sci. 2021, DOI: 10.1016/j.tips.2021.10.011

Antimicrobial 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/10.1101/2021.06.30.45046

Genome-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.02088-21

Downsizing antibodies: Towards complementarity-determining region (CDR)-based peptide mimetics

Van holsbeeck, K.; Martins, J. C.; Ballet, S.; Bioorganic Chemistry, 2021, 105563.

Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional mu/delta-Opioid Agonist–Neurokinin Antagonist Peptidomimetics

Gadais, C.; Piekielna-Ciesielska, J.; De Neve, J.; Martin, C.; Janecka, A.; Ballet, S. Molecules 2021, 26(17), 5406

Neuromedin U induces an invasive phenotype in CRC cells expressing the NMUR2 receptor

Przygodzka, P.; Sochacka, E.; Soboska, K.; Pacholczyk, M.; Papiewska-Pająk, I.; Przygodzki, T.; Płociński, P.; Ballet, S.; De Prins, A.; Boncela, J. J Exp Clin Cancer Res 2021, 40, 283

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, 689006

Efficient Synthesis of Polysubstituted 1,5-Benzodiazepinone Dipeptide Mimetics via an Ugi-4CR-Ullmann Condensation Sequence

Van Den Hauwe, R.; Elsocht, M.; Hollanders, C.; Ballet, S., Synlett, 2021, DOI: 10.1055/a-1545-2860

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, 57, 6863-6866

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, 12, 828-870

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, 60, 10247.

Constraining 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., 2021, 64, 9, 5345–5364

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), 635

Structure-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, 357–369

Anti-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, 12929–12941

Peptide-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, 406

Mechanistic 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), 912

Zn-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, 10, 7, 4280–4289

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, e3194

Solid-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.

A New Wave of Amide Bond Formations for Peptide Synthesis

Hollanders, K.; Maes, B. U.W.; Ballet, S. Synthesis, 2019, 51(11), 2261-2277.

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, 1317-1323

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.

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.

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.

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.

Injectable Peptide Hydrogels for Controlled Drug Release.

Mannes, M.; Martin, C.; Dumitrascuta, M.; Van Wanseele, Y.; Hernot, S.; Van Eeckhaut, A.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., J. Pept. Sci. 2018, 24, S159-S159.

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.

Modulating peptide hydrogel strength through halogenation.

Vandeplassche, W.; Ballet, S.; Martin, C.; Hoogenboom, R.; Madder, A., J. Pept. Sci. 2018, 24, S109-S110.

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, 2320-2323

Nanobody-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.

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.

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.

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, 1495

χ-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...

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

Zhu, Y.-P.; Mampuys, P.; Sergeyev, S.; Ballet, S.; Maes, B. U. W., 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.

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.

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.

Development 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.

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-S84

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. 2016, 59, 3777-3792.

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. W.; Janssens, F.; Ceusters, M.; Sommen, F.; Meert, T.; Przewlocka, B.; Tourwe, D.; Ballet, S., ACS Med. Chem. Lett. 2015, 6, 1209-1214.

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. W.; Tourwe, D.; Ballet, S., Eur. J. Med. Chem 2015, 92, 64-77.

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. H.; Barty, A.; Chapman, H. N.; Basu, S.; Coe, J.; Conrad, C. E.; Fromme, R.; Fromme, P.; Tourwé, D.; Schiller, P. W.; Roth, B. L.; Ballet, S.; Katritch, V.; Stevens, R. C.; Cherezov, V., Nat Struct Mol Biol 2015, 22, 265-268.

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, e110038

Rational 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-S208

Efficient 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.

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.

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.

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.

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.

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.

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.

Multiple Ligands in Opioid Research.

Ballet, S.; Pietsch, M.; Abell, A. D., Protein Pep. Lett. 2008, 15, 668-682.

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.

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

Azetidomonamide and Diazetidomonapyridone Metabolites Control Biofilm Formation and Pigment Synthesis in Pseudomonas aeruginosa

Ernst, S.; Volkov, A.N.; Stark, M.; Hölscher, L.; Steinert, K.; Fetzner, S.; Hennecke, U.; Drees, S.L.; J. Am. Chem. Soc. 2022, 144, 7676-7685

Brønsted Acid-Catalyzed Enantioselective Iodocycloetherification Enabled by Triphenylphosphine Selenide Cocatalysis

Guria, S.; Daniliuc, C.G.; Hennecke, U.; Adv. Synth. Catal. 2021, 363, 3852-3858.

A dynamic picture of the halolactonization reaction through a combination of ab initio metadynamics and experimental investigations

Van Lommel, R.; Bock, J.: Daniliuc, C.G.; Hennecke, U.; De Proft, F.; 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

Sartor, P.; Bock, J.; Hennecke, U., Thierbach, S.; Fetzner, S., FEBS J. 2021, 288, 2360-2376.

Enantioselective Dihalogenation of Alkenes

Bock, J.; Guria, S.; Wedek, V.; Hennecke, U., 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.

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.

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.

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.

Revealing the Positive Side of Fluorine

U. Hennecke, Science 2013, 340, 41-42.

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

Wandering beyond small molecules: peptides as allosteric protein modulators

Mannes, M.; Martin, C.; Menet, C.; Ballet, S. Trends Pharmacol. Sci. 2021, DOI: 10.1016/j.tips.2021.10.011

Harnessing the Anti-Nociceptive Potential of NK2 and NK3 Ligands in the Design of New Multifunctional mu/delta-Opioid Agonist–Neurokinin Antagonist Peptidomimetics

Gadais, C.; Piekielna-Ciesielska, J.; De Neve, J.; Martin, C.; Janecka, A.; Ballet, S. Molecules 2021, 26(17), 5406

Towards the understanding of halogenation in peptide hydrogels: a quantum chemical approach.

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, 60, 10247.

Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure

Anti-human PD-L1 Nanobody for Immuno-PET Imaging: Validation of a Conjugation Strategy for Clinical Translation

Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies

Peptide-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), 912

Zn-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, 10, 7, 4280–4289

Elucidating the active δ-opioid receptor crystal structure with peptide and small-molecule agonists.

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.

Radiometal-labeled anti-VCAM-1 nanobodies as molecular tracers for atherosclerosis – impact of radiochemistry on pharmacokinetics.

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.

A Bifunctional Biased Mu Opioid Agonist - Neuropeptide FF Receptor Antagonist as Analgesic with Improved Acute and Chronic Side Effects.

Injectable Peptide Hydrogels for Controlled Drug Release.

Mannes, M.; Martin, C.; Dumitrascuta, M.; Van Wanseele, Y.; Hernot, S.; Van Eeckhaut, A.; Madder, A.; Hoogenboom, R.; Spetea, M.; Ballet, S., J. Pept. Sci. 2018, 24, S159-S159.

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.

Modulating peptide hydrogel strength through halogenation.

Vandeplassche, W.; Ballet, S.; Martin, C.; Hoogenboom, R.; Madder, A., J. Pept. Sci. 2018, 24, S109-S110.

Biodegradable Amphipathic Peptide Hydrogels as Extended-Release System for Opioid Peptides.

A bifunctional-biased mu-opioid agonist-neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects.

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.

Rational Design of Nanobody80 Loop Peptidomimetics: Towards Biased beta(2) Adrenergic Receptor Ligands.

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. Chem. 2017, 292, 13097-13110.

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.

Injectable peptide-based hydrogel formulations for the extended in vivo release of opioids.

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.

Development 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.

Towards β-arrestin biased β2AR ligands: Rational Design of Nanobody Loop Mimetics.

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-S84

Silicon-Containing Amino Acids: Synthetic Aspects, Conformational Studies, and Applications to Bioactive Peptides.

Remond, E.; Martin, C.; Martinez, J.; Cavelier, F., Chem. Rev. 2016, 116, 11654-11684.

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