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Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Schönherr H, Ayaz P, Taylor AM, Casaletto JB, Touré BB, Moustakas DT, Hudson BM, Valverde R, Zhao S, O'Hearn PJ, Foster L, Sharon DA, Garfinkle S, Giordanetto F, Lescarbeau A, Kurukulasuriya R, Gerami-Moayed N, Maglic D, Bruderek K, Naik G, Gunaydin H, Mader MM, Boezio AA, McLean TH, Chen R, Wang Y, Shaw DE, Watters J, Bergstrom DA. Schönherr H, et al. Among authors: mclean th. Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. doi: 10.1073/pnas.2317756121. Epub 2024 Feb 1. Proc Natl Acad Sci U S A. 2024. PMID: 38300868 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. Among authors: mclean th. 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.
Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.
Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski NP, Lewis TA, Maglathin RL, McLean TH, Bochkarev A, Plotnikov AN, Vedadi M, Arrowsmith CH. Schuetz A, et al. Among authors: mclean th. J Biol Chem. 2008 Apr 25;283(17):11355-63. doi: 10.1074/jbc.M707362200. Epub 2008 Feb 19. J Biol Chem. 2008. PMID: 18285338 Free PMC article.