Literature DB >> 12646029

New active series of growth hormone secretagogues.

Vincent Guerlavais1, Damien Boeglin, Delphine Mousseaux, Catherine Oiry, Annie Heitz, Romano Deghenghi, Vittorio Locatelli, Antonio Torsello, Corrado Ghé, Filomena Catapano, Giampiero Muccioli, Jean-Claude Galleyrand, Jean-Alain Fehrentz, Jean Martinez.   

Abstract

New growth hormone secretagogue (GHS) analogues were synthesized and evaluated for growth hormone releasing activity. This series derived from EP-51389 is based on a gem-diamino structure. Compounds that exhibited higher in vivo GH-releasing potency than hexarelin in rat (subcutaneous administration) were then tested per os in beagle dogs and for their binding affinity to human pituitary GHS receptors and to hGHS-R 1a. Compound 7 (JMV 1843, H-Aib-(d)-Trp-(d)-gTrp-formyl) showed high potency in these tests and was selected for clinical studies.(1)

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Year:  2003        PMID: 12646029     DOI: 10.1021/jm020985q

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  16 in total

1.  Agonism, Antagonism, and Inverse Agonism Bias at the Ghrelin Receptor Signaling.

Authors:  Céline M'Kadmi; Jean-Philippe Leyris; Lauriane Onfroy; Céline Galés; Aude Saulière; Didier Gagne; Marjorie Damian; Sophie Mary; Mathieu Maingot; Séverine Denoyelle; Pascal Verdié; Jean-Alain Fehrentz; Jean Martinez; Jean-Louis Banères; Jacky Marie
Journal:  J Biol Chem       Date:  2015-09-11       Impact factor: 5.157

2.  Regulation of ERK1/2 activity by ghrelin-activated growth hormone secretagogue receptor 1A involves a PLC/PKCvarepsilon pathway.

Authors:  Delphine Mousseaux; Lionel Le Gallic; Joanne Ryan; Catherine Oiry; Didier Gagne; Jean-Alain Fehrentz; Jean-Claude Galleyrand; Jean Martinez
Journal:  Br J Pharmacol       Date:  2006-06       Impact factor: 8.739

3.  Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor.

Authors:  Sophie Mary; Marjorie Damian; Maxime Louet; Nicolas Floquet; Jean-Alain Fehrentz; Jacky Marie; Jean Martinez; Jean-Louis Banères
Journal:  Proc Natl Acad Sci U S A       Date:  2012-05-09       Impact factor: 11.205

Review 4.  Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases.

Authors:  Rasha Mofeed Habeeb Mosa; Zhen Zhang; Renfu Shao; Chao Deng; Jiezhong Chen; Chen Chen
Journal:  Endocrine       Date:  2015-02-04       Impact factor: 3.633

5.  A general alkyl-alkyl cross-coupling enabled by redox-active esters and alkylzinc reagents.

Authors:  Tian Qin; Josep Cornella; Chao Li; Lara R Malins; Jacob T Edwards; Shuhei Kawamura; Brad D Maxwell; Martin D Eastgate; Phil S Baran
Journal:  Science       Date:  2016-04-21       Impact factor: 47.728

Review 6.  The ghrelin axis in disease: potential therapeutic indications.

Authors:  Ralf Nass; Bruce D Gaylinn; Michael O Thorner
Journal:  Mol Cell Endocrinol       Date:  2011-02-25       Impact factor: 4.102

7.  Ghrelin stimulation of growth hormone-releasing hormone neurons is direct in the arcuate nucleus.

Authors:  Guillaume Osterstock; Pauline Escobar; Violeta Mitutsova; Laurie-Anne Gouty-Colomer; Pierre Fontanaud; François Molino; Jean-Alain Fehrentz; Danielle Carmignac; Jean Martinez; Nathalie C Guerineau; Iain C A F Robinson; Patrice Mollard; Pierre-François Méry
Journal:  PLoS One       Date:  2010-02-11       Impact factor: 3.240

8.  Protective but not anticonvulsant effects of ghrelin and JMV-1843 in the pilocarpine model of Status epilepticus.

Authors:  Chiara Lucchi; Giulia Curia; Jonathan Vinet; Fabio Gualtieri; Elena Bresciani; Vittorio Locatelli; Antonio Torsello; Giuseppe Biagini
Journal:  PLoS One       Date:  2013-08-28       Impact factor: 3.240

Review 9.  Targeting the ghrelin receptor: orally active GHS and cortistatin analogs.

Authors:  Romano Deghenghi; Fabio Broglio; Mauro Papotti; Giampiero Muccioli; Ezio Ghigo
Journal:  Endocrine       Date:  2003-10       Impact factor: 3.925

Review 10.  Neuroactive peptides as putative mediators of antiepileptic ketogenic diets.

Authors:  Carmela Giordano; Maddalena Marchiò; Elena Timofeeva; Giuseppe Biagini
Journal:  Front Neurol       Date:  2014-04-29       Impact factor: 4.003

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