Development and Pharmacological Characterization of Conformationally Constrained Urotensin II-Related Peptide Agonists

Autor: Debby Feytens, Nicolas Doucet, Myriam Létourneau, Alain Fournier, David Chatenet, Dirk Tourwé, Benjamin Folch

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, American Chemical Society, 2013, 56 (23), pp.9612-22. ⟨10.1021/jm401153j⟩

International audience; Urotensin II (UII) and its paralog peptide, urotensin II-related peptide (URP), exert not only common but also divergent actions through the activation of UT, a specific membrane-bound receptor that belongs to the 1A G protein

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6ed22156caba7761d09c5c1f2ad4f2c
https://doi.org/10.1021/jm401153j

Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds

Autor: Andrew D. Abell, Gianfranco Balboni, Severo Salvadori, Steven Ballet, Lawrence H. Lazarus, Yusuke Sasaki, Ewa D. Marczak, Debby Feytens, Dirk Tourwé

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1610-1613

The dimerization and trimerization of the Dmt-Tic, Dmt-Aia and Dmt-Aba pharmacophores provided multiple ligands which were evaluated in vitro for opioid receptor binding and functional activity. Whereas the Tic- and Aba multimers proved to be dual an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f815de246c4a848512b66dd7e92923ea
https://doi.org/10.1016/j.bmcl.2010.01.055

Influence of ring substitution on the conformation and β-turn mimicry of 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one peptide mimetics

Autor: Zofia Urbańczyk-Lipkowska, Rien De Wachter, Debby Feytens, Isabelle Van den Eynde, Steven Ballet, Attila Keresztes, Géza Tóth, Dirk Tourwé, Luc Brans

Publikováno v: Tetrahedron. 65:2266-2278

Analogs of 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-ones, containing a methyl substituent at the 4- or 5-position, or a phenyl substituent at C-1, were prepared. Conformational analysis of tetrapeptide models containing these analogs indicated diffe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ea8f9428c0c27c743eed1c794b2a3d49
https://doi.org/10.1016/j.tet.2009.01.057

Synthesis of 4-amino-3-oxo-tetrahydroazepino[3,4-b]indoles: new conformationally constrained Trp analogs

Autor: Debby Feytens, Dirk Tourwé, Nga N. Chung, Aleksandra Misicka, Karolina Pulka, Andrzej W. Lipkowski, Rien De Wachter, Piotr Kosson, Isabelle Van den Eynde, Peter W. Schiller

Publikováno v: Tetrahedron. 63:1459-1466

The synthesis of tryptophan analogs is reported in which the conformation has been constrained by formation of a seven-membered lactam. Boc-protected 2′-formyl tryptophan was obtained by SeO2 oxidation of Boc-tetrahydro-β-carboline-3-carboxylic ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::584ff2df4821429e45e0196321acf1ca
https://doi.org/10.1016/j.tet.2006.11.069

Conformational properties of peptides incorporating a fluorinated pseudoproline residue

Autor: Grégory Chaume, Thierry Brigaud, Solange Lavielle, Gérard Chassaing, Debby Feytens, Emeric Miclet

Publikováno v: New Journal of Chemistry
New Journal of Chemistry, 2013, 37 (5), pp.1336-1342. ⟨10.1039/c3nj41084f⟩
New Journal of Chemistry, Royal Society of Chemistry, 2013, 37 (5), pp.1336-1342. ⟨10.1039/c3nj41084f⟩

International audience; We have recently reported the synthesis of enantiomerically pure CF3-oxazolidine pseudoprolines (CF3-Psi Pro). Complete NMR studies, together with DFT calculations, have highlighted the marked stereoelectronic effects of the C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52414028139d294218d63ad1600f32ad
https://hal.science/hal-01366405