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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: williams rl. 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 p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.
Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Rückle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL. Berndt A, et al. Among authors: williams o, williams rl. Nat Chem Biol. 2010 Feb;6(2):117-24. doi: 10.1038/nchembio.293. Nat Chem Biol. 2010. PMID: 20081827 Free PMC article.
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: williams rl. 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: williams rl. Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683. Nat Commun. 2017. PMID: 28276440 Free PMC article.
887 results