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Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα.
Borsari C, Keles E, McPhail JA, Schaefer A, Sriramaratnam R, Goch W, Schaefer T, De Pascale M, Bal W, Gstaiger M, Burke JE, Wymann MP. Borsari C, et al. Among authors: burke je. J Am Chem Soc. 2022 Apr 13;144(14):6326-6342. doi: 10.1021/jacs.1c13568. Epub 2022 Mar 30. J Am Chem Soc. 2022. PMID: 35353516 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: burke je. 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: burke je. Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683. Nat Commun. 2017. PMID: 28276440 Free PMC article.
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Rageot D, Bohnacker T, Melone A, Langlois JB, Borsari C, Hillmann P, Sele AM, Beaufils F, Zvelebil M, Hebeisen P, Löscher W, Burke J, Fabbro D, Wymann MP. Rageot D, et al. J Med Chem. 2018 Nov 21;61(22):10084-10105. doi: 10.1021/acs.jmedchem.8b01262. Epub 2018 Nov 14. J Med Chem. 2018. PMID: 30359003 Free article.
Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.
Castro-Falcón G, Seiler GS, Demir Ö, Rathinaswamy MK, Hamelin D, Hoffmann RM, Makowski SL, Letzel AC, Field SJ, Burke JE, Amaro RE, Hughes CC. Castro-Falcón G, et al. Among authors: burke je. J Med Chem. 2018 Dec 13;61(23):10463-10472. doi: 10.1021/acs.jmedchem.8b00975. Epub 2018 Nov 28. J Med Chem. 2018. PMID: 30380865 Free PMC article.
158 results