Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

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., Larivée, A., LaRochelle, J. R., … Kipp, D. R. (2023). Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia. Cancer Discovery, 14(2), 240–257. https://doi.org/10.1158/2159-8290.cd-23-0944
Authors:
Andreas Varkaris
Ermira Pazolli
Hakan Gunaydin
Qi Wang
Levi Pierce
Alessandro A Boezio
Artemisa Bulku
Lucian DiPietro
Cary Fridrich
Adam Frost
Fabrizio Giordanetto
Erika P Hamilton
Katherine Harris
Michael Holliday
Tamieka L Hunter
Amanda Iskandar
Yongli Ji
Alexandre Larivée
Jonathan R LaRochelle
André Lescarbeau
Fabien Llambi
Brenda Lormil
Mary M Mader
Brenton G Mar
Iain Martin
Thomas H McLean
Klaus Michelsen
Yakov Pechersky
Erika Puente-Poushnejad
Kevin Raynor
Dipali Rogala
Ramin Samadani
Alison M Schram
Kelley Shortsleeves
Sweta Swaminathan
Shahein Tajmir
Gege Tan
Yong Tang
Roberto Valverde
Bryan Wehrenberg
Jeremy Wilbur
Bret R Williams
Hongtao Zeng
Hanmo Zhang
W Patrick Walters
Beni B Wolf
David E Shaw
Donald A Bergstrom
James Watters
James S Fraser
Pascal D Fortin
D Randal Kipp
Affiliated Authors:
David E Shaw
Columbia Affiliation:
Subjects:
Breast Neoplasms (MeSH)
Hyperinsulinism (MeSH)
elink
Publication Type:
Article
Unique ID:
10.1158/2159-8290.cd-23-0944
PMID:
37916956
DOI:
10.1158/2159-8290.cd-23-0944
Journal:
Cancer Discovery
Publication Date:
Data Source:
PubMed
Source Link:
View PubMed Record

Record Created: