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Approach to the specificity and selectivity between D2 and D3 receptors by mutagenesis and binding experiments part I: Expression and characterization of D2 and D3 receptor mutants

Autor: Céline, Legros, Anne, Rojas, Clémence, Dupré, Chantal, Brasseur, Isabelle, Riest-Fery, Olivier, Muller, Jean-Claude, Ortuno, Olivier, Nosjean, Sophie-Pénélope, Guenin, Gilles, Ferry, Jean A, Boutin

Publikováno v: Protein science : a publication of the Protein Society. 31(12)

D3/D2 sub-specificity is a complex problem to solve. Indeed, in the absence of easy structural biology of the G-protein coupled receptors, and despite key progresses in this area, the systematic knowledge of the ligand/receptor relationship is diffic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::dc1121ec1d7b67bf067023180e1d39df
https://pubmed.ncbi.nlm.nih.gov/36177735

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Deep generative models for ligand-based de novo design applied to multi-parametric optimization

Autor: Quentin Perron, Olivier Mirguet, Hamza Tajmouati, Adam Skiredj, Anne Rojas, Arnaud Gohier, Pierre Ducrot, Marie-Pierre Bourguignon, Patricia Sansilvestri-Morel, Nicolas Do Huu, Françoise Gellibert, Yann Gaston-Mathé

Publikováno v: Journal of computational chemistryREFERENCES. 43(10)

Multi-parameter optimization (MPO) is a major challenge in new chemical entity (NCE) drug discovery. Recently, promising results were reported for deep learning generative models applied to de novo molecular design, but, to our knowledge, until now n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::028ac16384184e88d4be6b26edbf9602
https://pubmed.ncbi.nlm.nih.gov/35218219

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Design and synthesis of novel N-sulfonyl-2-indoles that behave as 5-HT6 receptor ligands with significant selectivity for D3 over D2 receptors

Autor: Millan Mark, Stephen Hanessian, Oscar Mario Saavedra, Jean-Claude Ortuno, Delphine Dupuis, Arnaud Gohier, Clotilde Mannoury la Cour, Anne Rojas, Dominique Brossard, Delphine Karila

Publikováno v: Bioorganic & Medicinal Chemistry. 25:38-52

All clinically-used antipsychotics display similar affinity for both D2 (D2R) and D3 (D3R) receptors, and they likewise act as 5-HT2A receptor antagonists. They provide therapeutic benefit for positive symptoms, but no marked or consistent improvemen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1b2e9933b4136694c252b0a9208bf634
https://doi.org/10.1016/j.bmc.2016.10.010

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Present understanding of the relationship between exercise and arrhythmogenic right ventricular dysplasia/cardiomyopathy

Autor: Hugh Calkins, Anne Rojas

Publikováno v: Trends in Cardiovascular Medicine. 25:181-188

Arrhythmogenic right ventricular dysplasia/cardiomyopathy (ARVD/C) is an inherited cardiomyopathy that is characterized clinically by ventricular arrhythmias and an increased risk of sudden death and pathologically by fibrofatty replacement of the my

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::471ce9e52b764714fe6b69e20a2231a5
https://doi.org/10.1016/j.tcm.2014.10.007

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Synthesis of a new structural analogue of (+)-porothramycin

Autor: Anne Rojas-Rousseau, Nicole Langlois

Publikováno v: Tetrahedron. 57:3389-3395

A new phosphonate analogue of (+)-porothramycin has been synthesized from (S)-pyroglutaminol. Circular dichroism of diastereomeric intermediates 9 has been studied. The cytostatic activity of the new pyrrolo[2,1-c][1,4]benzodiazepine has been evaluat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::839d0322103e65dde9ee4909cbcbc70a
https://doi.org/10.1016/s0040-4020(01)00197-1

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Synthesis of conformationally constrained analogues of (R)-2-amino-7-phosphonoheptanoic acid

Autor: Oreste Decavallas, Anne Rojas-Rousseau, Nicole Langlois

Publikováno v: Tetrahedron: Asymmetry. 7:1095-1100

Conformationally restricted AP7 analogues of 2 R configuration are readily prepared from ( S )-pyroglutamic acid.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::277478cfb8e0e13f4c3a79688442b6a0
https://doi.org/10.1016/0957-4166(96)00114-0

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Synthesis of (2S,4S) 2-carboxy-4-pyrrolidine acetic acid, a conformationally constrained 2-amino adipic acid analogue

Autor: Nicole Langlois, Anne Rojas

Publikováno v: Tetrahedron Letters. 34:2477-2480

(2S,4S) 2-carboxy-4-pyrrolidine acetic acid was synthesized from (S) pyroglutamaic acid in 26% overall yield by a regiospecific deprotonation of the N-methoxycarbonyl benzylester 4.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cc82af16bc642ade1ff532af1ddf42fe
https://doi.org/10.1016/s0040-4039(00)60445-8

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A short synthesis of C-2 symmetric (2S, 5S) pyrrolidine-2,5 dicarboxylic acid, a constituent of red alga Schizymenia dubyi

Autor: Nicole Langlois, Anne Rojas

Publikováno v: Tetrahedron. 49:77-82

(2S, 5S) pyrrolidine-2,5-dicarboxylic acid 1 was synthesized from (5S) N-methoxycarbonyl-5-ethoxyethoxy-methyl pyrrolidin-2-one 2 by a simple and efficient way. 1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5659b051346c2824f47c74b00c35e108
https://doi.org/10.1016/s0040-4020(01)80507-x

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