8TGD

STX-478, a Mutant-Selective, Allosteric Inhibitor bound to H1047R PI3Kalpha

Summary for 8TGD

Entry DOI	10.2210/pdb8tgd/pdb
Related	8TDU
Descriptor	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, 1,2-ETHANEDIOL, ... (6 entities in total)
Functional Keywords	kinase, inhibitor, transferase, transferase-transferse inhibitor complex, transferase/transferse inhibitor
Biological source	Homo sapiens (human) More
Total number of polymer chains	4
Total formula weight	321755.82
Authors	Hilbert, B.,Brooijmans, N.,Buckbinder, L.,St.Jean Jr., D.J. (deposition date: 2023-07-12, release date: 2023-09-06, Last modification date: 2023-11-08)
Primary citation	Buckbinder, L.,St Jean Jr., D.J.,Tieu, T.,Ladd, B.,Hilbert, B.,Wang, W.,Alltucker, J.T.,Manimala, S.,Kryukov, G.V.,Brooijmans, N.,Dowdell, G.,Jonsson, P.,Huff, M.,Guzman-Perez, A.,Jackson, E.L.,Goncalves, M.D.,Stuart, D.D. STX-478, a Mutant-Selective, Allosteric PI3K alpha Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3K alpha-Mutant Xenografts. Cancer Discov, 13:2432-2447, 2023 Cited by PubMed: 37623743 DOI: 10.1158/2159-8290.CD-23-0396 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.928 Å)

Structure validation