8W9A

CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-7909 binding at an allosteric site

Summary for 8W9A

Entry DOI	10.2210/pdb8w9a/pdb
EMDB information	37362
Descriptor	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, 6-chloranyl-3-[[(1R)-1-[2-(1,3-dihydropyrrolo[3,4-c]pyridin-2-yl)-3,6-dimethyl-4-oxidanylidene-quinazolin-8-yl]ethyl]amino]pyridine-2-carboxylic acid, ... (4 entities in total)
Functional Keywords	pi3k-alpha, lipid kinase, allosteric inhibition, oncoprotein
Biological source	Homo sapiens (human) More
Total number of polymer chains	2
Total formula weight	208431.97
Authors	Huang, X.,Ren, X.,Zhong, W. (deposition date: 2023-09-05, release date: 2024-04-17)
Primary citation	Huang, X.,Wang, K.,Han, J.,Chen, X.,Wang, Z.,Wu, T.,Yu, B.,Zhao, F.,Wang, X.,Li, H.,Xie, Z.,Zhu, X.,Zhong, W.,Ren, X. Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop. Structure, 2024 Cited by PubMed: 38582077 DOI: 10.1016/j.str.2024.03.007 PDB entries with the same primary citation
Experimental method	ELECTRON MICROSCOPY (2.7 Å)

Structure validation