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Discovery, Structure-Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5.
Picon S, Boulahjar R, Hoguet V, Baron M, Duplan I, Vallez E, Hennuyer N, Dumont J, Touche V, Dorchies E, Lasalle M, Descat A, Piveteau C, Biela A, Chaput L, Villoutreix BO, Lipka E, Sevin E, Culot M, Gosselet F, Lestavel S, Roussel P, Deprez-Poulain R, Leroux F, Staels B, Deprez B, Tailleux A, Charton J. Picon S, et al. Among authors: deprez poulain r. J Med Chem. 2023 Sep 14;66(17):11732-11760. doi: 10.1021/acs.jmedchem.2c01881. Epub 2023 Aug 28. J Med Chem. 2023. PMID: 37639383
Facts, figures and trends in lead generation.
Deprez-Poulain R, Deprez B. Deprez-Poulain R, et al. Curr Top Med Chem. 2004;4(6):569-80. doi: 10.2174/1568026043451168. Curr Top Med Chem. 2004. PMID: 14965294 Review.
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.
Maingot L, Elbakali J, Dumont J, Bosc D, Cousaert N, Urban A, Deglane G, Villoutreix B, Nagase H, Sperandio O, Leroux F, Deprez B, Deprez-Poulain R. Maingot L, et al. Eur J Med Chem. 2013 Nov;69:244-61. doi: 10.1016/j.ejmech.2013.08.027. Epub 2013 Aug 30. Eur J Med Chem. 2013. PMID: 24044937
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis.
Charton J, Gauriot M, Guo Q, Hennuyer N, Marechal X, Dumont J, Hamdane M, Pottiez V, Landry V, Sperandio O, Flipo M, Buee L, Staels B, Leroux F, Tang WJ, Deprez B, Deprez-Poulain R. Charton J, et al. Eur J Med Chem. 2014 May 22;79:184-93. doi: 10.1016/j.ejmech.2014.04.009. Epub 2014 Apr 4. Eur J Med Chem. 2014. PMID: 24735644 Free PMC article.
Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.
Charton J, Gauriot M, Totobenazara J, Hennuyer N, Dumont J, Bosc D, Marechal X, Elbakali J, Herledan A, Wen X, Ronco C, Gras-Masse H, Heninot A, Pottiez V, Landry V, Staels B, Liang WG, Leroux F, Tang WJ, Deprez B, Deprez-Poulain R. Charton J, et al. Eur J Med Chem. 2015 Jan 27;90:547-67. doi: 10.1016/j.ejmech.2014.12.005. Epub 2014 Dec 4. Eur J Med Chem. 2015. PMID: 25489670 Free PMC article.
37 results