Synthesis and Pharmacological in Vitro and in Vivo Evaluations of Novel Triazole Derivatives as Ligands of the Ghrelin Receptor. 1

Autor: Didier Gagne, Antonio Torsello, Aline Moulin, Jean Claude Galleyrand, Jean-Alain Fehrentz, Delphine Mousseaux, Daniel Perrissoud, Annie Heitz, Luc Demange, Damien Boeglin, Vittorio Locatelli, Jean Martinez, Gilbert Bergé, Joanne Ryan

Publikováno v: Journal of Medicinal Chemistry. 50:1939-1957

A new series of growth hormone secretagogue (GHS) analogues based on the 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and their ability to stimulate intracellular calcium release to the cloned hGHS-1a ghrelin rec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::117e0b6f6a59fc4f8a033f8f7d84d2c2
https://doi.org/10.1021/jm070024h

Design and Synthesis of Potent Bradykinin Agonists Containing a Benzothiazepine Moiety

Autor: Jean Martinez, Pierre Bélichard, Jean-Luc Paquet, Pierre Dodey, Didier Pruneau, Gilbert Bergé, Isabelle Daffix, Philippe Bedos, Muriel Amblard, Jean-Michel Luccarini

Publikováno v: Journal of Medicinal Chemistry. 42:4185-4192

A bradykinin analogue (H-Arg-Pro-Pro-Gly-Phe-Ser-D-BT-Arg-OH, 3) in which the Pro-Phe dipeptide was replaced by the (3S)[amino]-5-(carbonylmethyl)-2,3-dihydro-1, 5-benzothiazepin-4(5H)-one (D-BT) moiety has been synthesized. The same modification was

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe1c133b8ba3c3e1b1343a027cbfa637
https://doi.org/10.1021/jm9901529

Involvement of tryptophan W276 and of two surrounding amino acid residues in the high constitutive activity of the ghrelin receptor GHS-R1a

Autor: Nicolas Floquet, Jean-Alain Fehrentz, Catherine Gozé, Gilbert Bergé, Jean-Claude Galleyrand, Céline M'Kadmi, Didier Gagne, Jean Martinez

Publikováno v: European Journal of Pharmacology Molecular Pharmacology
European Journal of Pharmacology Molecular Pharmacology, Elsevier, 2010, 643 (2-3), pp.153-161. ⟨10.1016/j.ejphar.2010.06.018⟩

642NO Times Cited:0 Cited References Count:30; The human ghrelin receptor (GHS-R1a) is known to display a high level of signaling in the absence of ligand. The Trp276, located in the fully conserved CWXP motif of G protein-coupled receptors, is belie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb725ae239bc38a1162a2dc047a8a082
https://hal.archives-ouvertes.fr/hal-00583009

Solid-phase synthesis of dipeptidic and pseudo-dipeptidic potential NOS inhibitors through a side-chain anchoring approach

Autor: Youness, Touati-Jallabe, Abdallah, Hamzé, Gilbert, Bergé, Claudia, Verna, Anne-Dominique, Lajoix, Pierre, Fulcrand, Jean, Martinez, Jean-François, Hernandez

Publikováno v: Advances in experimental medicine and biology. 611

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::884c2421b7c96c04773b7624b06e6b8c
https://pubmed.ncbi.nlm.nih.gov/19400126

Design, synthesis, and biological evaluation of 1,5-benzothiazepine-4-one derivatives targeting factor VIIa/tissue factor

Autor: Pierre Fulcrand, Philippe Gloanec, Philippe Mennecier, Jean Martinez, Gilbert Bergé, Jean-François Hernandez, Alain Rupin, Erwan Ayral, Tony Verbeuren, Guillaume De Nanteuil

Publikováno v: Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (5), pp.1386-1391. ⟨10.1016/j.bmcl.2009.01.039⟩

414UR Times Cited:0 Cited References Count:43; The 1,5-benzothiazepine-4-one scaffold was earlier shown to provide efficient protease inhibitors. In this contribution, we describe its use in the design of factor VIIa/tissue factor inhibitors. A serie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4920ba8c71c1daae63c453b41f9c7f68
https://hal.archives-ouvertes.fr/hal-00389293