8OW2

Crystal structure of the p110alpha catalytic subunit from homo sapiens in complex with activator 1938

Replaces:  8BFV

Summary for 8OW2

• Entry DOI: 10.2210/pdb8ow2/pdb
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, 1-[7-[[2-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyridin-4-yl]amino]-2,3-dihydroindol-1-yl]ethanone (3 entities in total)
• Functional Keywords: cardioprotection, neuroregeneration, pi3k, kinase, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 110425.65

Authors

Gong, G.Q.,Bellini, D.,Vanhaesebroeck, B.,Williams, R.L. (deposition date: 2023-04-26, release date: 2023-05-24, Last modification date: 2023-06-07)

• Primary citation: Gong, G.Q.,Bilanges, B.,Allsop, B.,Masson, G.R.,Roberton, V.,Askwith, T.,Oxenford, S.,Madsen, R.R.,Conduit, S.E.,Bellini, D.,Fitzek, M.,Collier, M.,Najam, O.,He, Z.,Wahab, B.,McLaughlin, S.H.,Chan, A.W.E.,Feierberg, I.,Madin, A.,Morelli, D.,Bhamra, A.,Vinciauskaite, V.,Anderson, K.E.,Surinova, S.,Pinotsis, N.,Lopez-Guadamillas, E.,Wilcox, M.,Hooper, A.,Patel, C.,Whitehead, M.A.,Bunney, T.D.,Stephens, L.R.,Hawkins, P.T.,Katan, M.,Yellon, D.M.,Davidson, S.M.,Smith, D.M.,Phillips, J.B.,Angell, R.,Williams, R.L.,Vanhaesebroeck, B.; A small-molecule PI3K alpha activator for cardioprotection and neuroregeneration.; Nature, 618:159-168, 2023; PubMed: 37225977; DOI: 10.1038/s41586-023-05972-2

Experimental method

X-RAY DIFFRACTION (2.57 Å)