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Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo.
Dubiella C, Pinch BJ, Koikawa K, Zaidman D, Poon E, Manz TD, Nabet B, He S, Resnick E, Rogel A, Langer EM, Daniel CJ, Seo HS, Chen Y, Adelmant G, Sharifzadeh S, Ficarro SB, Jamin Y, Martins da Costa B, Zimmerman MW, Lian X, Kibe S, Kozono S, Doctor ZM, Browne CM, Yang A, Stoler-Barak L, Shah RB, Vangos NE, Geffken EA, Oren R, Koide E, Sidi S, Shulman Z, Wang C, Marto JA, Dhe-Paganon S, Look T, Zhou XZ, Lu KP, Sears RC, Chesler L, Gray NS, London N. Dubiella C, et al. Among authors: pinch bj. Nat Chem Biol. 2021 Sep;17(9):954-963. doi: 10.1038/s41589-021-00786-7. Epub 2021 May 10. Nat Chem Biol. 2021. PMID: 33972797 Free PMC article.
Identification of a potent and selective covalent Pin1 inhibitor.
Pinch BJ, Doctor ZM, Nabet B, Browne CM, Seo HS, Mohardt ML, Kozono S, Lian X, Manz TD, Chun Y, Kibe S, Zaidman D, Daitchman D, Yeoh ZC, Vangos NE, Geffken EA, Tan L, Ficarro SB, London N, Marto JA, Buratowski S, Dhe-Paganon S, Zhou XZ, Lu KP, Gray NS. Pinch BJ, et al. Nat Chem Biol. 2020 Sep;16(9):979-987. doi: 10.1038/s41589-020-0550-9. Epub 2020 Jun 1. Nat Chem Biol. 2020. PMID: 32483379 Free PMC article.
Development and Characterization of a Wee1 Kinase Degrader.
Li Z, Pinch BJ, Olson CM, Donovan KA, Nowak RP, Mills CE, Scott DA, Doctor ZM, Eleuteri NA, Chung M, Sorger PK, Fischer ES, Gray NS. Li Z, et al. Among authors: pinch bj. Cell Chem Biol. 2020 Jan 16;27(1):57-65.e9. doi: 10.1016/j.chembiol.2019.10.013. Epub 2019 Nov 14. Cell Chem Biol. 2020. PMID: 31735695 Free PMC article.
Targeting Pin1 renders pancreatic cancer eradicable by synergizing with immunochemotherapy.
Koikawa K, Kibe S, Suizu F, Sekino N, Kim N, Manz TD, Pinch BJ, Akshinthala D, Verma A, Gaglia G, Nezu Y, Ke S, Qiu C, Ohuchida K, Oda Y, Lee TH, Wegiel B, Clohessy JG, London N, Santagata S, Wulf GM, Hidalgo M, Muthuswamy SK, Nakamura M, Gray NS, Zhou XZ, Lu KP. Koikawa K, et al. Among authors: pinch bj. Cell. 2021 Sep 2;184(18):4753-4771.e27. doi: 10.1016/j.cell.2021.07.020. Epub 2021 Aug 12. Cell. 2021. PMID: 34388391 Free PMC article.
A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes.
Pinch BJ, Buckley DL, Gleim S, Brittain SM, Tandeske L, D'Alessandro PL, Hauseman ZJ, Lipps J, Xu L, Harvey EP, Schirle M, Sprague ER, Forrester WC, Dovala D, McGregor LM, Thoma CR. Pinch BJ, et al. Cell Chem Biol. 2022 Jan 20;29(1):57-66.e6. doi: 10.1016/j.chembiol.2021.08.007. Epub 2021 Sep 8. Cell Chem Biol. 2022. PMID: 34499862 Free article.
A Novel Bifunctional Alkylphenol Anesthetic Allows Characterization of γ-Aminobutyric Acid, Type A (GABAA), Receptor Subunit Binding Selectivity in Synaptosomes.
Woll KA, Murlidaran S, Pinch BJ, Hénin J, Wang X, Salari R, Covarrubias M, Dailey WP, Brannigan G, Garcia BA, Eckenhoff RG. Woll KA, et al. Among authors: pinch bj. J Biol Chem. 2016 Sep 23;291(39):20473-86. doi: 10.1074/jbc.M116.736975. Epub 2016 Jul 26. J Biol Chem. 2016. PMID: 27462076 Free PMC article.