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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: wang w, wang j. 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. Among authors: wang j. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.
Bondeson DP, Smith BE, Burslem GM, Buhimschi AD, Hines J, Jaime-Figueroa S, Wang J, Hamman BD, Ishchenko A, Crews CM. Bondeson DP, et al. Among authors: wang j. Cell Chem Biol. 2018 Jan 18;25(1):78-87.e5. doi: 10.1016/j.chembiol.2017.09.010. Epub 2017 Nov 9. Cell Chem Biol. 2018. PMID: 29129718 Free PMC article.
Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases.
Steinig AG, Li AH, Wang J, Chen X, Dong H, Ferraro C, Jin M, Kadalbajoo M, Kleinberg A, Stolz KM, Tavares-Greco PA, Wang T, Albertella MR, Peng Y, Crew L, Kahler J, Kan J, Schulz R, Cooke A, Bittner M, Turton RW, Franklin M, Gokhale P, Landfair D, Mantis C, Workman J, Wild R, Pachter J, Epstein D, Mulvihill MJ. Steinig AG, et al. Among authors: wang j, wang t. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4381-7. doi: 10.1016/j.bmcl.2013.05.074. Epub 2013 May 30. Bioorg Med Chem Lett. 2013. PMID: 23773865
Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: optimization of kinase selectivity and pharmacokinetics.
Hornberger KR, Chen X, Crew AP, Kleinberg A, Ma L, Mulvihill MJ, Wang J, Wilde VL, Albertella M, Bittner M, Cooke A, Kadhim S, Kahler J, Maresca P, May E, Meyn P, Romashko D, Tokar B, Turton R. Hornberger KR, et al. Among authors: wang j. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4511-6. doi: 10.1016/j.bmcl.2013.06.054. Epub 2013 Jun 27. Bioorg Med Chem Lett. 2013. PMID: 23856049
Imidazo[1,5-a]pyrazines: orally efficacious inhibitors of mTORC1 and mTORC2.
Crew AP, Bhagwat SV, Dong H, Bittner MA, Chan A, Chen X, Coate H, Cooke A, Gokhale PC, Honda A, Jin M, Kahler J, Mantis C, Mulvihill MJ, Tavares-Greco PA, Volk B, Wang J, Werner DS, Arnold LD, Pachter JA, Wild R, Gibson NW. Crew AP, et al. Among authors: wang j. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2092-7. doi: 10.1016/j.bmcl.2011.01.139. Epub 2011 Feb 3. Bioorg Med Chem Lett. 2011. PMID: 21353551
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