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KRAS G12C fragment screening renders new binding pockets.
Mathieu M, Steier V, Fassy F, Delorme C, Papin D, Genet B, Duffieux F, Bertrand T, Delarbre L, Le-Borgne H, Parent A, Didier P, Marquette JP, Lowinski M, Houtmann J, Lamberton A, Debussche L, Alexey R. Mathieu M, et al. Among authors: steier v. Small GTPases. 2022 Jan;13(1):225-238. doi: 10.1080/21541248.2021.1979360. Epub 2021 Sep 24. Small GTPases. 2022. PMID: 34558391 Free PMC article.
Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.
El-Ahmad Y, Tabart M, Halley F, Certal V, Thompson F, Filoche-Rommé B, Gruss-Leleu F, Muller C, Brollo M, Fabien L, Loyau V, Bertin L, Richepin P, Pilorge F, Desmazeau P, Girardet C, Beccari S, Louboutin A, Lebourg G, Le-Roux J, Terrier C, Vallée F, Steier V, Mathieu M, Rak A, Abecassis PY, Vicat P, Benard T, Bouaboula M, Sun F, Shomali M, Hebert A, Levit M, Cheng H, Courjaud A, Ginesty C, Perrault C, Garcia-Echeverria C, McCort G, Schio L. El-Ahmad Y, et al. Among authors: steier v. J Med Chem. 2020 Jan 23;63(2):512-528. doi: 10.1021/acs.jmedchem.9b01293. Epub 2019 Nov 27. J Med Chem. 2020. PMID: 31721572
The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1.
Amaning K, Lowinski M, Vallee F, Steier V, Marcireau C, Ugolini A, Delorme C, Foucalt F, McCort G, Derimay N, Andouche C, Vougier S, Llopart S, Halland N, Rak A. Amaning K, et al. Among authors: steier v. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3620-6. doi: 10.1016/j.bmcl.2013.04.003. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23648182