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EMD-41617
CryoEM structure of PI3Kalpha
EMD-41617
Single-particle3.12 Å
Deposition: 15/08/2023Map released: 15/11/2023
Last modified: 28/05/2025
Sample Organism:
Homo sapiens
Sample: PI3Kalpha
Fitted models: 8tu6
Deposition Authors: Valverde R
,
Shi H,
Holliday M ,
Sun M
Sample: PI3Kalpha
Fitted models: 8tu6
Deposition Authors: Valverde R
,
Shi H,
Holliday M ,
Sun M
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.
Varkaris A ,
Pazolli E ,
Gunaydin H ,
Wang Q ,
Pierce L ,
Boezio AA ,
Bulku A,
DiPietro L ,
Fridrich C,
Frost A ,
Giordanetto F ,
Hamilton EP ,
Harris K ,
Holliday M ,
Hunter TL ,
Iskandar A ,
Ji Y ,
Larivee A ,
LaRochelle JR ,
Lescarbeau A ,
Llambi F ,
Lormil B ,
Mader MM ,
Mar BG ,
Martin I ,
McLean TH ,
Michelsen K ,
Pechersky Y ,
Puente-Poushnejad E ,
Raynor K,
Rogala D,
Samadani R ,
Schram AM ,
Shortsleeves K ,
Swaminathan S ,
Tajmir S ,
Tan G ,
Tang Y ,
Valverde R ,
Wehrenberg B ,
Wilbur J ,
Williams BR ,
Zeng H ,
Zhang H,
Walters WP ,
Wolf BB ,
Shaw DE ,
Bergstrom DA ,
Watters J ,
Fraser JS ,
Fortin PD ,
Kipp DR
(2024) Cancer Discov , 14 , 240 - 257
,
Pazolli E ,
Gunaydin H ,
Wang Q ,
Pierce L ,
Boezio AA ,
Bulku A,
DiPietro L ,
Fridrich C,
Frost A ,
Giordanetto F ,
Hamilton EP ,
Harris K ,
Holliday M ,
Hunter TL ,
Iskandar A ,
Ji Y ,
Larivee A ,
LaRochelle JR ,
Lescarbeau A ,
Llambi F ,
Lormil B ,
Mader MM ,
Mar BG ,
Martin I ,
McLean TH ,
Michelsen K ,
Pechersky Y ,
Puente-Poushnejad E ,
Raynor K,
Rogala D,
Samadani R ,
Schram AM ,
Shortsleeves K ,
Swaminathan S ,
Tajmir S ,
Tan G ,
Tang Y ,
Valverde R ,
Wehrenberg B ,
Wilbur J ,
Williams BR ,
Zeng H ,
Zhang H,
Walters WP ,
Wolf BB ,
Shaw DE ,
Bergstrom DA ,
Watters J ,
Fraser JS ,
Fortin PD ,
Kipp DR
(2024) Cancer Discov , 14 , 240 - 257
Grant Support: