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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: chan e. 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.
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers.
Cantley J, Ye X, Rousseau E, Januario T, Hamman BD, Rose CM, Cheung TK, Hinkle T, Soto L, Quinn C, Harbin A, Bortolon E, Chen X, Haskell R, Lin E, Yu SF, Del Rosario G, Chan E, Dunlap D, Koeppen H, Martin S, Merchant M, Grimmer M, Broccatelli F, Wang J, Pizzano J, Dragovich PS, Berlin M, Yauch RL. Cantley J, et al. Among authors: chan e. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs.
Zhang D, Ma B, Dragovich PS, Ma L, Chen S, Chen EC, Ye X, Liu J, Pizzano J, Bortolon E, Chan E, Zhang X, Chen YC, Levy ES, Yauch RL, Khojasteh SC, Hop CECA. Zhang D, et al. Among authors: chan e. Commun Med (Lond). 2024 May 16;4(1):87. doi: 10.1038/s43856-024-00505-y. Commun Med (Lond). 2024. PMID: 38755248 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: chan ew. 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
Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry.
Tran JC, Hunsaker T, Bell C, Ma TP, Chan E, Larrocha PS, Homyk K, Liu L, La H, Mao J, de la Cruz CC, Yu K, Beresini M, Forrest WF, Xiao Y, Jang A, Samus N, Stesco ND, Mentinova M, Parent S, Pottiez G, Schirm M, Purkey HE, Liu Y, Merchant M. Tran JC, et al. Among authors: chan e. Anal Chem. 2023 Mar 21;95(11):4834-4839. doi: 10.1021/acs.analchem.2c04417. Epub 2023 Mar 6. Anal Chem. 2023. PMID: 36876898
4,978 results