8AM0

Crystal structure of human T1061E PI3Kalpha in complex with its regulatory subunit and the inhibitor GDC-0077 (Inavolisib)

Summary for 8AM0

• Entry DOI: 10.2210/pdb8am0/pdb
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Isoform 3 of Phosphatidylinositol 3-kinase regulatory subunit alpha, (2R)-2-[[2-[(4S)-4-[bis(fluoranyl)methyl]-2-oxidanylidene-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]amino]propanamide, ... (7 entities in total)
• Functional Keywords: lipid kinase, phosphoinositide, 3-kinase, signaling, transferase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 160453.96

Authors

Goncalves, M.,Johnson, J.L.,Roewer, K.M. (deposition date: 2022-08-02, release date: 2023-12-13, Last modification date: 2024-01-03)

• Primary citation: Lin, T.Y.,Ramsamooj, S.,Perrier, T.,Liberatore, K.,Lantier, L.,Vasan, N.,Karukurichi, K.,Hwang, S.K.,Kesicki, E.A.,Kastenhuber, E.R.,Wiederhold, T.,Yaron, T.M.,Huntsman, E.M.,Zhu, M.,Ma, Y.,Paddock, M.N.,Zhang, G.,Hopkins, B.D.,McGuinness, O.,Schwartz, R.E.,Ersoy, B.A.,Cantley, L.C.,Johnson, J.L.,Goncalves, M.D.; Epinephrine inhibits PI3K alpha via the Hippo kinases.; Cell Rep, 42:113535-113535, 2023; PubMed: 38060450; DOI: 10.1016/j.celrep.2023.113535

Experimental method

X-RAY DIFFRACTION (2.818 Å)