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An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance.
Hagenbeek TJ, Zbieg JR, Hafner M, Mroue R, Lacap JA, Sodir NM, Noland CL, Afghani S, Kishore A, Bhat KP, Yao X, Schmidt S, Clausen S, Steffek M, Lee W, Beroza P, Martin S, Lin E, Fong R, Di Lello P, Kubala MH, Yang MN, Lau JT, Chan E, Arrazate A, An L, Levy E, Lorenzo MN, Lee HJ, Pham TH, Modrusan Z, Zang R, Chen YC, Kabza M, Ahmed M, Li J, Chang MT, Maddalo D, Evangelista M, Ye X, Crawford JJ, Dey A. Hagenbeek TJ, et al. Among authors: arrazate a. Nat Cancer. 2023 Jun;4(6):812-828. doi: 10.1038/s43018-023-00577-0. Epub 2023 Jun 5. Nat Cancer. 2023. PMID: 37277530 Free PMC article.
Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
Taylor AM, Williams BR, Giordanetto F, Kelley EH, Lescarbeau A, Shortsleeves K, Tang Y, Walters WP, Arrazate A, Bowman C, Brophy E, Chan EW, Deshmukh G, Greisman JB, Hunsaker TL, Kipp DR, Saenz Lopez-Larrocha P, Maddalo D, Martin IJ, Maragakis P, Merchant M, Murcko M, Nisonoff H, Nguyen V, Nguyen V, Orozco O, Owen C, Pierce L, Schmidt M, Shaw DE, Smith S, Therrien E, Tran JC, Watters J, Waters NJ, Wilbur J, Willmore L. Taylor AM, et al. Among authors: arrazate a. J Med Chem. 2023 Oct 12;66(19):13384-13399. doi: 10.1021/acs.jmedchem.3c00483. Epub 2023 Sep 29. J Med Chem. 2023. PMID: 37774359
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: arrazate a. Elife. 2016 Jul 13;5:e15828. doi: 10.7554/eLife.15828. Elife. 2016. PMID: 27410477 Free PMC article.
Correction: The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer.
Joseph JD, Darimont B, Zhou W, Arrazate A, Young A, Ingalla E, Walter K, Blake RA, Nonomiya J, Guan Z, Kategaya L, Govek SP, Lai AG, Kahraman M, Brigham D, Sensintaffar J, Lu N, Shao G, Qian J, Grillot K, Moon M, Prudente R, Bischoff E, Lee KJ, Bonnefous C, Douglas KL, Julien JD, Nagasawa JY, Aparicio A, Kaufman J, Haley B, Giltnane JM, Wertz IE, Lackner MR, Nannini MA, Sampath D, Schwarz L, Manning HC, Tantawy MN, Arteaga CL, Heyman RA, Rix PJ, Friedman L, Smith ND, Metcalfe C, Hager JH. Joseph JD, et al. Among authors: arrazate a. Elife. 2019 Jan 7;8:e44851. doi: 10.7554/eLife.44851. Elife. 2019. PMID: 30614786 Free PMC article.