New insights into the human 5-HT4receptor binding site: exploration of a hydrophobic pocket

Autor: Lucie Rivail, Bernard Maigret, Mireille Giner, Monique Gastineau, Isabelle Berque-Bestel, Frank Lezoualc'h, Sames Sicsic, Magali Berthouze, Rodolphe Fischmeister, Jean-Louis Soulier

Publikováno v: British Journal of Pharmacology. 143:361-370

A body of evidences suggests that a hydrophobic pocket of the human 5-HT4 receptor contributes to the high affinity of some bulky 5-HT4 ligands. A thorough study of this pocket was performed using mutagenesis and molecular modeling. Ligand binding or

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9db6caed5b198b1ab0daf29235e59f0a
https://doi.org/10.1038/sj.bjp.0705950

Two transmembrane Cys residues are involved in 5-HT4 receptor dimerization

Autor: Frank Lezoualc'h, Lucie Rivail, Sames Sicsic, Olivier Russo, Mohammed Akli Ayoub, Rodolphe Fischmeister, Alexandre Lucas, Isabelle Berque-Bestel, Ralf Jockers, Magali Berthouze

Publikováno v: Biochemical and Biophysical Research Communications
Biochemical and Biophysical Research Communications, Elsevier, 2007, 356 (3), pp.642-647. ⟨10.1016/j.bbrc.2007.03.030⟩

The 5-HT(4) receptor (5-HT(4)R) belongs to the G-protein-coupled receptor (GPCR) family and is of considerable interest for the development of new drugs to treat gastrointestinal diseases and memory disorders. The 5-HT(4)R exists as a constitutive di

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6025b4b84666ac580ac85a3c9552d58
https://pubmed.ncbi.nlm.nih.gov/17379184

Design and synthesis of specific probes for human 5-HT4 receptor dimerization studies

Autor: Bernard Maigret, Sames Sicsic, Lucie Rivail, Sandrine Ongeri, Frank Lezoualc'h, Rodolphe Fischmeister, Jean-Louis Soulier, Magali Berthouze, Olivier Russo, Isabelle Berque-Bestel, Mireille Giner

Publikováno v: Journal of medicinal chemistry. 48(20)

Recently, human 5-HT4 receptors have been demonstrated to form constitutive dimers in living cells. To evaluate the role of dimerization on the 5-HT4 receptor function, we investigated the conception and the synthesis of bivalent molecules able to in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5439429336236532be0ead8ef302a855
https://pubmed.ncbi.nlm.nih.gov/16190749

Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors

Autor: Mireille Giner, Lucie Rivail, Michel Langlois, J.L. Soulier, Sames Sicsic, Isabelle Berque-Bestel

Publikováno v: Journal of medicinal chemistry. 46(13)

Fluorescent antagonists for human 5-HT(4) receptors were synthesized based on ML10302 1, a potent 5-HT(4) receptor agonist and on piperazine analogue 2. These molecules were derived with three fluorescent moieties, dansyl, naphthalimide, and NBD (7-n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11385c55b3e954c8a0e2f858c06a0479
https://pubmed.ncbi.nlm.nih.gov/12801225

Constitutive dimerization of human serotonin 5-HT4 receptors in living cells

Autor: Lucie Rivail, Rodolphe Fischmeister, Ralf Jockers, Magali Berthouze, Frank Lezoualc'h, Mohammed Akli Ayoub, Olivier Russo, Sames Sicsic, Isabelle Berque-Bestel

Publikováno v: FEBS Letters. (14):2973-2980

Serotonin 5-HT4 receptor isoforms are G protein-coupled receptors (GPCRs) with distinct pharmacological properties and may represent a valuable target for the treatment of many human disorders. Here, we have explored the process of dimerization of hu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d9dd60323358cc159b2334c84482c5b