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Correction to "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, Crew AP, Davenport K, DiNicola D, Dong H, 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, Snyder LB, Soto L, Staben LR, Sun H, Tian Q, Wang G, Wang J, Wang W, Ye CS, Ye X, Zhang P, Zhou Y, Yauch R, Dragovich PS. Berlin M, et al. Among authors: haskell r. J Med Chem. 2025 Jun 12;68(11):12284. doi: 10.1021/acs.jmedchem.5c01287. Epub 2025 May 21. J Med Chem. 2025. PMID: 40395158 No abstract available.
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: haskell r. 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: haskell r. Nat Commun. 2022 Nov 10;13(1):6814. doi: 10.1038/s41467-022-34562-5. Nat Commun. 2022. PMID: 36357397 Free PMC article.
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Regueiro-Ren A, Sit SY, Chen Y, Chen J, Swidorski JJ, Liu Z, Venables BL, Sin N, Hartz RA, Protack T, Lin Z, Zhang S, Li Z, Wu DR, Li P, Kempson J, Hou X, Gupta A, Rampulla R, Mathur A, Park H, Sarjeant A, Benitex Y, Rahematpura S, Parker D, Phillips T, Haskell R, Jenkins S, Santone KS, Cockett M, Hanumegowda U, Dicker I, Meanwell NA, Krystal M. Regueiro-Ren A, et al. Among authors: haskell r. J Med Chem. 2022 Sep 22;65(18):11927-11948. doi: 10.1021/acs.jmedchem.2c00879. Epub 2022 Aug 31. J Med Chem. 2022. PMID: 36044257
Structure-Property Basis for Solving Transporter-Mediated Efflux and Pan-Genotypic Inhibition in HCV NS5B Inhibitors.
Yeung KS, Beno BR, Mosure K, Zhu J, Grant-Young KA, Parcella K, Anjanappa P, Bora RO, Selvakumar K, Wang YK, Fang H, Krause R, Rigat K, Liu M, Lemm J, Sheriff S, Witmer M, Tredup J, Jardel A, Kish K, Parker D, Haskell R, Santone K, Meanwell NA, Soars MG, Roberts SB, Kadow JF. Yeung KS, et al. Among authors: haskell r. ACS Med Chem Lett. 2018 Nov 5;9(12):1217-1222. doi: 10.1021/acsmedchemlett.8b00379. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613329 Free PMC article.
Linking (Pyr)1apelin-13 pharmacokinetics to efficacy: Stabilization and measurement of a high clearance peptide in rodents.
Onorato JM, Xu C, Chen XQ, Rose AV, Generaux C, Lentz K, Shipkova P, Arthur S, Hennan JK, Haskell R, Myers MC, Lawrence RM, Finlay HJ, Basso M, Bostwick J, Fernando G, Garcia R, Hellings S, Hsu MY, Zhang R, Zhao L, Gargalovic P. Onorato JM, et al. Among authors: haskell r. Anal Biochem. 2019 Mar 1;568:41-50. doi: 10.1016/j.ab.2018.12.022. Epub 2018 Dec 31. Anal Biochem. 2019. PMID: 30605634
Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1 R,3a S,5a R,5b R,7a R,11a S,11b R,13a R,13b R)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1 H-cyclopenta[ a]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176).
Regueiro-Ren A, Swidorski JJ, Liu Z, Chen Y, Sin N, Sit SY, Chen J, Venables BL, Zhu J, Nowicka-Sans B, Protack T, Lin Z, Terry B, Samanta H, Zhang S, Li Z, Easter J, Beno BR, Arora V, Huang XS, Rahematpura S, Parker DD, Haskell R, Santone KS, Cockett MI, Krystal M, Meanwell NA, Jenkins S, Hanumegowda U, Dicker IB. Regueiro-Ren A, et al. Among authors: haskell r. J Med Chem. 2018 Aug 23;61(16):7289-7313. doi: 10.1021/acs.jmedchem.8b00854. Epub 2018 Aug 1. J Med Chem. 2018. PMID: 30067361
120 results