8TDU
STX-478, a Mutant-Selective, Allosteric Inhibitor bound to PI3Kalpha
Summary for 8TDU
Entry DOI | 10.2210/pdb8tdu/pdb |
Descriptor | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, N~2~-{(4S,11aP)-2-[(4S)-4-(difluoromethyl)-2-oxo-1,3-oxazolidin-3-yl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl}-L-alaninamide, ... (5 entities in total) |
Functional Keywords | kinase, inhibitor, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (human) More |
Total number of polymer chains | 4 |
Total formula weight | 320910.84 |
Authors | Hilbert, B.J.,Brooijmans, N.,Buckbinder, L.,St.Jean Jr., D.J. (deposition date: 2023-07-05, 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: 37623743DOI: 10.1158/2159-8290.CD-23-0396 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (3.11 Å) |
Structure validation
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