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Allosteric PI3Kα Inhibition Overcomes On-target Resistance to Orthosteric Inhibitors Mediated by Secondary PIK3CA Mutations.
Varkaris A, Fece de la Cruz F, Martin EE, Norden BL, Chevalier N, Kehlmann AM, Leshchiner I, Barnes H, Ehnstrom S, Stavridi AM, Yuan X, Kim JS, Ellis H, Papatheodoridi A, Gunaydin H, Danysh BP, Parida L, Sanidas I, Ji Y, Lau K, Wulf GM, Bardia A, Spring LM, Isakoff SJ, Lennerz JK, Del Vecchio K, Pierce L, Pazolli E, Getz G, Corcoran RB, Juric D. Varkaris A, et al. Cancer Discov. 2024 Feb 8;14(2):227-239. doi: 10.1158/2159-8290.CD-23-0704. Cancer Discov. 2024. PMID: 37916958 Free PMC article.
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. 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.
Plk1 Inhibitors and Abiraterone Synergistically Disrupt Mitosis and Kill Cancer Cells of Disparate Origin Independently of Androgen Receptor Signaling.
Patterson JC, Varkaris A, Croucher PJP, Ridinger M, Dalrymple S, Nouri M, Xie F, Varmeh S, Jonas O, Whitman MA, Chen S, Rashed S, Makusha L, Luo J, Isaacs JT, Erlander MG, Einstein DJ, Balk SP, Yaffe MB. Patterson JC, et al. Among authors: varkaris a. Cancer Res. 2023 Jan 18;83(2):219-238. doi: 10.1158/0008-5472.CAN-22-1533. Cancer Res. 2023. PMID: 36413141 Free PMC article.
EGFR-A763_Y764insFQEA Is a Unique Exon 20 Insertion Mutation That Displays Sensitivity to Approved and In-Development Lung Cancer EGFR Tyrosine Kinase Inhibitors.
Vasconcelos PENS, Gergis C, Viray H, Varkaris A, Fujii M, Rangachari D, VanderLaan PA, Kobayashi IS, Kobayashi SS, Costa DB. Vasconcelos PENS, et al. Among authors: varkaris a. JTO Clin Res Rep. 2020 Sep;1(3):100051. doi: 10.1016/j.jtocrr.2020.100051. Epub 2020 May 13. JTO Clin Res Rep. 2020. PMID: 34104899 Free PMC article.
33 results