8GUB

Cryo-EM structure of cancer-specific PI3Kalpha mutant H1047R in complex with BYL-719

Summary for 8GUB

Entry DOI	10.2210/pdb8gub/pdb
EMDB information	34272
Descriptor	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, (2S)-N~1~-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide (3 entities in total)
Functional Keywords	phosphoinositide 3-kinase (pi3k), kinase domain, mutation, cancers, structural protein
Biological source	Homo sapiens (human) More
Total number of polymer chains	2
Total formula weight	211906.30
Authors	Liu, X.,Zhou, Q.,Hart, J.R.,Xu, Y.,Yang, S.,Yang, D.,Vogt, P.K.,Wang, M.-W. (deposition date: 2022-09-11, release date: 2022-11-23)
Primary citation	Liu, X.,Zhou, Q.,Hart, J.R.,Xu, Y.,Yang, S.,Yang, D.,Vogt, P.K.,Wang, M.W. Cryo-EM structures of cancer-specific helical and kinase domain mutations of PI3K alpha. Proc.Natl.Acad.Sci.USA, 119:e2215621119-e2215621119, 2022 Cited by PubMed: 36343266 DOI: 10.1073/pnas.2215621119 PDB entries with the same primary citation
Experimental method	ELECTRON MICROSCOPY (2.73 Å)

Structure validation