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A class of highly selective inhibitors bind to an active state of PI3Kγ.
Gangadhara G, Dahl G, Bohnacker T, Rae R, Gunnarsson J, Blaho S, Öster L, Lindmark H, Karabelas K, Pemberton N, Tyrchan C, Mogemark M, Wymann MP, Williams RL, Perry MWD, Papavoine T, Petersen J. Gangadhara G, et al. Among authors: wymann mp. Nat Chem Biol. 2019 Apr;15(4):348-357. doi: 10.1038/s41589-018-0215-0. Epub 2019 Feb 4. Nat Chem Biol. 2019. PMID: 30718815
The chemical biology of phosphoinositide 3-kinases.
Wymann MP, Schultz C. Wymann MP, et al. Chembiochem. 2012 Sep 24;13(14):2022-35. doi: 10.1002/cbic.201200089. Epub 2012 Sep 10. Chembiochem. 2012. PMID: 22965647 Review.
PKCβ phosphorylates PI3Kγ to activate it and release it from GPCR control.
Walser R, Burke JE, Gogvadze E, Bohnacker T, Zhang X, Hess D, Küenzi P, Leitges M, Hirsch E, Williams RL, Laffargue M, Wymann MP. Walser R, et al. Among authors: wymann mp. PLoS Biol. 2013;11(6):e1001587. doi: 10.1371/journal.pbio.1001587. Epub 2013 Jun 25. PLoS Biol. 2013. PMID: 23824069 Free PMC article.
Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.
Bohnacker T, Prota AE, Beaufils F, Burke JE, Melone A, Inglis AJ, Rageot D, Sele AM, Cmiljanovic V, Cmiljanovic N, Bargsten K, Aher A, Akhmanova A, Díaz JF, Fabbro D, Zvelebil M, Williams RL, Steinmetz MO, Wymann MP. Bohnacker T, et al. Among authors: wymann mp. Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683. Nat Commun. 2017. PMID: 28276440 Free PMC article.
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Beaufils F, Cmiljanovic N, Cmiljanovic V, Bohnacker T, Melone A, Marone R, Jackson E, Zhang X, Sele A, Borsari C, Mestan J, Hebeisen P, Hillmann P, Giese B, Zvelebil M, Fabbro D, Williams RL, Rageot D, Wymann MP. Beaufils F, et al. Among authors: wymann mp. J Med Chem. 2017 Sep 14;60(17):7524-7538. doi: 10.1021/acs.jmedchem.7b00930. Epub 2017 Sep 1. J Med Chem. 2017. PMID: 28829592 Free PMC article.
131 results