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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 AA, Bulku A, DiPietro L, Fridrich C, Frost A, Giordanetto F, Hamilton EP, Harris K, Holliday M, Hunter TL, Iskandar A, Ji Y, Larivée 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. Varkaris A, et al. Among authors: larivee a. Cancer Discov. 2024 Feb 8;14(2):240-257. doi: 10.1158/2159-8290.CD-23-0944. Cancer Discov. 2024. PMID: 37916956 Free PMC article.
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Beveridge RE, Wallweber HA, Ashkenazi A, Beresini M, Clark KR, Gibbons P, Ghiro E, Kaufman S, Larivée A, Leblanc M, Leclerc JP, Lemire A, Ly C, Rudolph J, Schwarz JB, Srivastava S, Wang W, Zhao L, Braun MG. Beveridge RE, et al. Among authors: larivee a. ACS Med Chem Lett. 2020 Oct 16;11(12):2389-2396. doi: 10.1021/acsmedchemlett.0c00344. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335661 Free PMC article.
The leiodolide B puzzle.
Larivée A, Unger JB, Thomas M, Wirtz C, Dubost C, Handa S, Fürstner A. Larivée A, et al. Angew Chem Int Ed Engl. 2011 Jan 3;50(1):304-9. doi: 10.1002/anie.201005850. Angew Chem Int Ed Engl. 2011. PMID: 21082641 No abstract available.
12 results