8TU6

CryoEM structure of PI3Kalpha

Summary for 8TU6

• Entry DOI: 10.2210/pdb8tu6/pdb
• EMDB information: 41617
• Descriptor: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha (2 entities in total)
• Functional Keywords: pi3kalapha, isoform selective, structure-based drug design., cytosolic protein
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 210012.27

Authors

Valverde, R.,Shi, H.,Holliday, M. (deposition date: 2023-08-15, release date: 2023-11-15, Last modification date: 2024-02-21)

• Primary citation: Varkaris, A.,Pazolli, E.,Gunaydin, H.,Wang, Q.,Pierce, L.,Boezio, A.A.,Bulku, A.,DiPietro, L.,Fridrich, C.,Frost, A.,Giordanetto, F.,Hamilton, E.P.,Harris, K.,Holliday, M.,Hunter, T.L.,Iskandar, A.,Ji, Y.,Larivee, A.,LaRochelle, J.R.,Lescarbeau, A.,Llambi, F.,Lormil, B.,Mader, M.M.,Mar, B.G.,Martin, I.,McLean, T.H.,Michelsen, K.,Pechersky, Y.,Puente-Poushnejad, E.,Raynor, K.,Rogala, D.,Samadani, R.,Schram, A.M.,Shortsleeves, K.,Swaminathan, S.,Tajmir, S.,Tan, G.,Tang, Y.,Valverde, R.,Wehrenberg, B.,Wilbur, J.,Williams, B.R.,Zeng, H.,Zhang, H.,Walters, W.P.,Wolf, B.B.,Shaw, D.E.,Bergstrom, D.A.,Watters, J.,Fraser, J.S.,Fortin, P.D.,Kipp, D.R.; Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3K alpha Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.; Cancer Discov, 14:240-257, 2024; PubMed: 37916956; DOI: 10.1158/2159-8290.CD-23-0944

Experimental method

ELECTRON MICROSCOPY (3.12 Å)