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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: london n. 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.
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. Among authors: london n. 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.
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: london n. 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.
Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor.
Shraga A, Olshvang E, Davidzohn N, Khoshkenar P, Germain N, Shurrush K, Carvalho S, Avram L, Albeck S, Unger T, Lefker B, Subramanyam C, Hudkins RL, Mitchell A, Shulman Z, Kinoshita T, London N. Shraga A, et al. Among authors: london n. Cell Chem Biol. 2019 Jan 17;26(1):98-108.e5. doi: 10.1016/j.chembiol.2018.10.011. Epub 2018 Nov 15. Cell Chem Biol. 2019. PMID: 30449673 Free article.
Hitting KRAS When It's Down.
Gabizon R, London N. Gabizon R, et al. Among authors: london n. J Med Chem. 2020 Jul 9;63(13):6677-6678. doi: 10.1021/acs.jmedchem.0c00785. Epub 2020 Jun 22. J Med Chem. 2020. PMID: 32568546 Free PMC article.
Covalent docking of large libraries for the discovery of chemical probes.
London N, Miller RM, Krishnan S, Uchida K, Irwin JJ, Eidam O, Gibold L, Cimermančič P, Bonnet R, Shoichet BK, Taunton J. London N, et al. Nat Chem Biol. 2014 Dec;10(12):1066-72. doi: 10.1038/nchembio.1666. Epub 2014 Oct 26. Nat Chem Biol. 2014. PMID: 25344815 Free PMC article.
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.
Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N. Resnick E, et al. Among authors: london n. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22. J Am Chem Soc. 2019. PMID: 31060360 Free PMC article.
Overcoming insecticide resistance through computational inhibitor design.
Correy GJ, Zaidman D, Harmelin A, Carvalho S, Mabbitt PD, Calaora V, James PJ, Kotze AC, Jackson CJ, London N. Correy GJ, et al. Among authors: london n. Proc Natl Acad Sci U S A. 2019 Oct 15;116(42):21012-21021. doi: 10.1073/pnas.1909130116. Epub 2019 Oct 1. Proc Natl Acad Sci U S A. 2019. PMID: 31575743 Free PMC article.
Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs.
Gabizon R, Shraga A, Gehrtz P, Livnah E, Shorer Y, Gurwicz N, Avram L, Unger T, Aharoni H, Albeck S, Brandis A, Shulman Z, Katz BZ, Herishanu Y, London N. Gabizon R, et al. Among authors: london n. J Am Chem Soc. 2020 Jul 8;142(27):11734-11742. doi: 10.1021/jacs.9b13907. Epub 2020 May 19. J Am Chem Soc. 2020. PMID: 32369353 Free PMC article.
658 results