5JHA

Structure of Phosphoinositide 3-kinase gamma (PI3K) bound to the potent inhibitor PIKin2

Summary for 5JHA

• Entry DOI: 10.2210/pdb5jha/pdb
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, [1-{4-[6-amino-4-(trifluoromethyl)pyridin-3-yl]-6-(morpholin-4-yl)pyrimidin-2-yl}-3-(chloromethyl)azetidin-3-yl]methanol, SULFATE ION, ... (4 entities in total)
• Functional Keywords: inhibitor, lipid kinase, pi3k, transferase
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm : P48736
• Total number of polymer chains: 1
• Total formula weight: 110741.32

Authors

Burke, J.E.,Inglis, A.J.,Williams, R.L. (deposition date: 2016-04-20, release date: 2017-03-15, Last modification date: 2024-01-10)

• Primary citation: Bohnacker, T.,Prota, A.E.,Beaufils, F.,Burke, J.E.,Melone, A.,Inglis, A.J.,Rageot, D.,Sele, A.M.,Cmiljanovic, V.,Cmiljanovic, N.,Bargsten, K.,Aher, A.,Akhmanova, A.,Diaz, J.F.,Fabbro, D.,Zvelebil, M.,Williams, R.L.,Steinmetz, M.O.,Wymann, M.P.; Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.; Nat Commun, 8:14683-14683, 2017; PubMed: 28276440; DOI: 10.1038/ncomms14683

Experimental method

X-RAY DIFFRACTION (2.51 Å)