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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: kerry ps. 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
Structural basis of SARM1 activation, substrate recognition, and inhibition by small molecules.
Shi Y, Kerry PS, Nanson JD, Bosanac T, Sasaki Y, Krauss R, Saikot FK, Adams SE, Mosaiab T, Masic V, Mao X, Rose F, Vasquez E, Furrer M, Cunnea K, Brearley A, Gu W, Luo Z, Brillault L, Landsberg MJ, DiAntonio A, Kobe B, Milbrandt J, Hughes RO, Ve T. Shi Y, et al. Among authors: kerry ps. Mol Cell. 2022 May 5;82(9):1643-1659.e10. doi: 10.1016/j.molcel.2022.03.007. Epub 2022 Mar 24. Mol Cell. 2022. PMID: 35334231 Free PMC article.
SARM1 is a metabolic sensor activated by an increased NMN/NAD+ ratio to trigger axon degeneration.
Figley MD, Gu W, Nanson JD, Shi Y, Sasaki Y, Cunnea K, Malde AK, Jia X, Luo Z, Saikot FK, Mosaiab T, Masic V, Holt S, Hartley-Tassell L, McGuinness HY, Manik MK, Bosanac T, Landsberg MJ, Kerry PS, Mobli M, Hughes RO, Milbrandt J, Kobe B, DiAntonio A, Ve T. Figley MD, et al. Among authors: kerry ps. Neuron. 2021 Apr 7;109(7):1118-1136.e11. doi: 10.1016/j.neuron.2021.02.009. Epub 2021 Mar 2. Neuron. 2021. PMID: 33657413 Free PMC article.
16 results