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PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models.
Berlin M, Cantley J, Bookbinder M, Bortolon E, Broccatelli F, Cadelina G, Chan EW, Chen H, Chen X, Cheng Y, Cheung TK, Davenport K, DiNicola D, Gordon D, Hamman BD, Harbin A, Haskell R, He M, Hole AJ, Januario T, Kerry PS, Koenig SG, Li L, Merchant M, Pérez-Dorado I, Pizzano J, Quinn C, Rose CM, Rousseau E, Soto L, Staben LR, Sun H, Tian Q, Wang J, Wang W, Ye CS, Ye X, Zhang P, Zhou Y, Yauch R, Dragovich PS. Berlin M, et al. Among authors: chan ew. J Med Chem. 2024 Jan 25;67(2):1262-1313. doi: 10.1021/acs.jmedchem.3c01781. Epub 2024 Jan 5. J Med Chem. 2024. PMID: 38180485
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. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 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. Anal Chem. 2023 Mar 21;95(11):4834-4839. doi: 10.1021/acs.analchem.2c04417. Epub 2023 Mar 6. Anal Chem. 2023. PMID: 36876898
Copolymers of Gelatin-graft-poly(3-hexylthiophene) for Transient Electronics.
Sun X, Chan EWC, Chen Q, Kirby N, Yang J, Mata JP, Kingston RL, Barker D, Domigan L, Travas-Sejdic J. Sun X, et al. Among authors: chan ewc. ACS Appl Mater Interfaces. 2024 Apr 26. doi: 10.1021/acsami.4c02174. Online ahead of print. ACS Appl Mater Interfaces. 2024. PMID: 38668737
584 results