Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies
Gonzalez, Simon, Dumitrascuta, Maria, Eiselt, Emilie, Louis, Stevany, Kunze, Linda, Blasiol, Annalisa, Vivancos, Mélanie, Previti, Santo, Dewolf, Elke, Martin, Charlotte, Tourwé, Dirk, Cavelier, Florine, Gendron, Louis, Sarret, Philippe, Spetea, Mariana, Ballet, Steven
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design
Gimenez, Luis E., Martin, Charlotte, Yu, Jing, Hollanders, Charlie, Hernandez, Ciria C., Wu, Yiran, Yao, Deqiang, Han, Gye Won, Dahir, Naima S., Wu, Lijie, Van der Poorten, Olivier, Lamouroux, Arthur, Mannes, Morgane, Zhao, Suwen, Tourwé, Dirk, Stevens, Raymond C., Cone, Roger D., Ballet, Steven
Published in Journal of medicinal chemistry (22.02.2024)
Published in Journal of medicinal chemistry (22.02.2024)
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Journal Article
Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia
Eiselt, Emilie, Gonzalez, Simon, Martin, Charlotte, Chartier, Magali, Betti, Cecilia, Longpré, Jean-Michel, Cavelier, Florine, Tourwé, Dirk, Gendron, Louis, Ballet, Steven, Sarret, Philippe
Published in ACS chemical neuroscience (20.11.2019)
Published in ACS chemical neuroscience (20.11.2019)
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Journal Article
Bifunctional Peptide-Based Opioid Agonist–Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain
Guillemyn, Karel, Starnowska, Joanna, Lagard, Camille, Dyniewicz, Jolanta, Rojewska, Ewelina, Mika, Joanna, Chung, Nga N, Utard, Valérie, Kosson, Piotr, Lipkowski, Andrzej W, Chevillard, Lucie, Arranz-Gibert, Pol, Teixidó, Meritxell, Megarbane, Bruno, Tourwé, Dirk, Simonin, Frédéric, Przewlocka, Barbara, Schiller, Peter W, Ballet, Steven
Published in Journal of medicinal chemistry (28.04.2016)
Published in Journal of medicinal chemistry (28.04.2016)
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Journal Article
Structural basis for bifunctional peptide recognition at human δ-opioid receptor
Fenalti, Gustavo, Zatsepin, Nadia A, Betti, Cecilia, Giguere, Patrick, Han, Gye Won, Ishchenko, Andrii, Liu, Wei, Guillemyn, Karel, Zhang, Haitao, James, Daniel, Wang, Dingjie, Weierstall, Uwe, Spence, John C H, Boutet, Sébastien, Messerschmidt, Marc, Williams, Garth J, Gati, Cornelius, Yefanov, Oleksandr M, White, Thomas A, Oberthuer, Dominik, Metz, Markus, Yoon, Chun Hong, Barty, Anton, Chapman, Henry N, Basu, Shibom, Coe, Jesse, Conrad, Chelsie E, Fromme, Raimund, Fromme, Petra, Tourwé, Dirk, Schiller, Peter W, Roth, Bryan L, Ballet, Steven, Katritch, Vsevolod, Stevens, Raymond C, Cherezov, Vadim
Published in Nature structural & molecular biology (01.03.2015)
Published in Nature structural & molecular biology (01.03.2015)
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Journal Article
Hybrid opioid/non-opioid ligands in pain research
Kleczkowska, Patrycja, Lipkowski, Andrzej W, Tourwé, Dirk, Ballet, Steven
Published in Current pharmaceutical design (01.12.2013)
Published in Current pharmaceutical design (01.12.2013)
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Journal Article
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure
Martin, Charlotte, Gimenez, Luis E., Williams, Savannah Y., Jing, Yu, Wu, Yiran, Hollanders, Charlie, Van der Poorten, Olivier, Gonzalez, Simon, Van Holsbeeck, Kevin, Previti, Santo, Lamouroux, Arthur, Zhao, Suwen, Tourwe, Dirk, Stevens, Raymond C., Cone, Roger D., Ballet, Steven
Published in Journal of medicinal chemistry (14.01.2021)
Published in Journal of medicinal chemistry (14.01.2021)
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Journal Article
Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice
Starnowska, Joanna, Costante, Roberto, Guillemyn, Karel, Popiolek-Barczyk, Katarzyna, Chung, Nga N, Lemieux, Carole, Keresztes, Attila, Van Duppen, Joost, Mollica, Adriano, Streicher, John, Vanden Broeck, Jozef, Schiller, Peter W, Tourwé, Dirk, Mika, Joanna, Ballet, Steven, Przewlocka, Barbara
Published in ACS chemical neuroscience (18.10.2017)
Published in ACS chemical neuroscience (18.10.2017)
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Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability
Tourwé, Dirk, Tsiailanis, Antonis D., Parisis, Nikolaos, Hirmiz, Baydaa, Del Borgo, Mark, Aguilar, Marie-Isabel, Van der Poorten, Olivier, Ballet, Steven, Widdop, Robert E., Tzakos, Andreas G.
Published in Bioorganic & medicinal chemistry letters (01.07.2021)
Published in Bioorganic & medicinal chemistry letters (01.07.2021)
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Novel DOTA-Neurotensin Analogues for 111In Scintigraphy and 68Ga PET Imaging of Neurotensin Receptor-Positive Tumors
Alshoukr, Faisal, Prignon, Aurélie, Brans, Luc, Jallane, Abdelhak, Mendes, Sandra, Talbot, Jean-Noël, Tourwé, Dirk, Barbet, Jacques, Gruaz-Guyon, Anne
Published in Bioconjugate chemistry (20.07.2011)
Published in Bioconjugate chemistry (20.07.2011)
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Journal Article
Design, Synthesis, and In Vitro Characterization of Proteolytically-Stable Opioid-Neurotensin Hybrid Peptidomimetics
De Neve, Jolien, Breault, Émile, Previti, Santo, Vangeloven, Esaü, Loranger, Bobbi, Chartier, Magali, Brouillette, Rebecca, Lanoie, Annik, Holleran, Brian J., Longpré, Jean-Michel, Gendron, Louis, Tourwé, Dirk, Sarret, Philippe, Ballet, Steven
Published in ACS pharmacology & translational science (13.09.2024)
Published in ACS pharmacology & translational science (13.09.2024)
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Journal Article
Development of potent and proteolytically stable human neuromedin U receptor agonists
De Prins, An, Martin, Charlotte, Van Wanseele, Yannick, Skov, Louise Julie, Tömböly, Csaba, Tourwé, Dirk, Caveliers, Vicky, Van Eeckhaut, Ann, Holst, Birgitte, Rosenkilde, Mette Marie, Smolders, Ilse, Ballet, Steven
Published in European journal of medicinal chemistry (20.01.2018)
Published in European journal of medicinal chemistry (20.01.2018)
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Journal Article
Trifluoromethylated Proline Surrogates as Part of “Pro–Pro” Turn‐Inducing Templates
Gadais, Charlène, Van holsbeeck, Kevin, Moors, Samuel L. C., Buyst, Dieter, Fehér, Krisztina, Van Hecke, Kristof, Tourwé, Dirk, Brigaud, Thierry, Martin, Charlotte, De Proft, Frank, Pytkowicz, Julien, Martins, José C., Chaume, Grégory, Ballet, Steven
Published in Chembiochem : a European journal of chemical biology (01.10.2019)
Published in Chembiochem : a European journal of chemical biology (01.10.2019)
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Journal Article
Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds
Dyniewicz, Jolanta, Lipiński, Piotr F. J, Kosson, Piotr, Leśniak, Anna, Bochyńska-Czyż, Marta, Muchowska, Adriana, Tourwé, Dirk, Ballet, Steven, Misicka, Aleksandra, Lipkowski, Andrzej W
Published in ACS medicinal chemistry letters (12.01.2017)
Published in ACS medicinal chemistry letters (12.01.2017)
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Variation of the Net Charge, Lipophilicity, and Side Chain Flexibility in Dmt1‑DALDA: Effect on Opioid Activity and Biodistribution
Novoa, Alexandre, Van Dorpe, Sylvia, Wynendaele, Evelien, Spetea, Mariana, Bracke, Nathalie, Stalmans, Sofie, Betti, Cecilia, Chung, Nga N, Lemieux, Carole, Zuegg, Johannes, Cooper, Matthew A, Tourwé, Dirk, De Spiegeleer, Bart, Schiller, Peter W, Ballet, Steven
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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Journal Article
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, Steven, Feytens, Debby, Buysse, Koen, Chung, Nga N, Lemieux, Carole, Tumati, Suneeta, Keresztes, Attila, Van Duppen, Joost, Lai, Josephine, Varga, Eva, Porreca, Frank, Schiller, Peter W, Vanden Broeck, Jozef, Tourwé, Dirk
Published in Journal of medicinal chemistry (14.04.2011)
Published in Journal of medicinal chemistry (14.04.2011)
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Journal Article
Design, Synthesis, Pharmacological Evaluation, and Structure−Activity Study of Novel Endomorphin Analogues with Multiple Structural Modifications
Mallareddy, Jayapal Reddy, Borics, Attila, Keresztes, Attila, Kövér, Katalin E, Tourwé, Dirk, Tóth, Géza
Published in Journal of medicinal chemistry (10.03.2011)
Published in Journal of medicinal chemistry (10.03.2011)
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Journal Article
Novel Neurotensin Analogues for Radioisotope Targeting to Neurotensin Receptor-Positive Tumors
Alshoukr, Faisal, Rosant, Cedric, Maes, Veronique, Abdelhak, Jallane, Raguin, Olivier, Burg, Samuel, Sarda, Laure, Barbet, Jacques, Tourwé, Dirk, Pelaprat, Didier, Gruaz-Guyon, Anne
Published in Bioconjugate chemistry (19.08.2009)
Published in Bioconjugate chemistry (19.08.2009)
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Journal Article
Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist – Neurokinin-1 antagonist peptidomimetics
Guillemyn, Karel, Kleczkowska, Patrycia, Lesniak, Anna, Dyniewicz, Jolanta, Van der Poorten, Olivier, Van den Eynde, Isabelle, Keresztes, Attila, Varga, Eva, Lai, Josephine, Porreca, Frank, Chung, Nga N., Lemieux, Carole, Mika, Joanna, Rojewska, Ewelina, Makuch, Wioletta, Van Duppen, Joost, Przewlocka, Barbara, Vanden Broeck, Jozef, Lipkowski, Andrzej W., Schiller, Peter W., Tourwé, Dirk, Ballet, Steven
Published in European journal of medicinal chemistry (06.03.2015)
Published in European journal of medicinal chemistry (06.03.2015)
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Journal Article
Indoloazepinone‐Constrained Oligomers as Cell‐Penetrating and Blood–Brain‐Barrier‐Permeating Compounds
Van der Poorten, Olivier, Legrand, Baptiste, Vezenkov, Lubomir L., García‐Pindado, Júlia, Bettache, Nadir, Knuhtsen, Astrid, Pedersen, Daniel Sejer, Sánchez‐Navarro, Macarena, Martinez, Jean, Teixidó, Meritxell, Garcia, Marcel, Tourwé, Dirk, Amblard, Muriel, Ballet, Steven
Published in Chembiochem : a European journal of chemical biology (04.04.2018)
Published in Chembiochem : a European journal of chemical biology (04.04.2018)
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