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Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.

Potter A, Oldfield V, Nunns C, Fromont C, Ray S, Northfield CJ, Bryant CJ, Scrace SF, Robinson D, Matossova N, Baker L, Dokurno P, Surgenor AE, Davis B, Richardson CM, Murray JB, Moore JD
Bioorg Med Chem Lett 20 6483-8 (2010)
Related entries: 2xp3, 2xp4, 2xp5, 2xp6, 2xp7, 2xp8, 2xp9, 2xpb, 3odk

Cited: 44 times
EuropePMC logo PMID: 20932746

Abstract

Pin1 is an emerging oncology target strongly implicated in Ras and ErbB2-mediated tumourigenesis. Pin1 isomerizes bonds linking phospho-serine/threonine moieties to proline enabling it to play a key role in proline-directed kinase signalling. Here we report a novel series of Pin1 inhibitors based on a phenyl imidazole acid core that contains sub-μM inhibitors. Compounds have been identified that block prostate cancer cell growth under conditions where Pin1 is essential.

Articles - 2xpa mentioned but not cited (2)

  1. The conserved npl4 protein complex mediates proteasome-dependent membrane-bound transcription factor activation. Hitchcock AL, Krebber H, Frietze S, Lin A, Latterich M, Silver PA. Mol Biol Cell 12 3226-3241 (2001)
  2. Exploring Ligand Stability in Protein Crystal Structures Using Binding Pose Metadynamics. Fusani L, Palmer DS, Somers DO, Wall ID. J Chem Inf Model 60 1528-1539 (2020)


Reviews citing this publication (11)

  1. Comprehensive review in current developments of imidazole-based medicinal chemistry. Zhang L, Peng XM, Damu GL, Geng RX, Zhou CH. Med Res Rev 34 340-437 (2014)
  2. The isomerase PIN1 controls numerous cancer-driving pathways and is a unique drug target. Zhou XZ, Lu KP. Nat Rev Cancer 16 463-478 (2016)
  3. Peptidyl-Proline Isomerases (PPIases): Targets for Natural Products and Natural Product-Inspired Compounds. Dunyak BM, Gestwicki JE. J Med Chem 59 9622-9644 (2016)
  4. Roles of Prolyl Isomerases in RNA-Mediated Gene Expression. Thapar R. Biomolecules 5 974-999 (2015)
  5. Structure and function of the human parvulins Pin1 and Par14/17. Matena A, Rehic E, Hönig D, Kamba B, Bayer P. Biol Chem 399 101-125 (2018)
  6. Function of PIN1 in Cancer Development and Its Inhibitors as Cancer Therapeutics. Yu JH, Im CY, Min SH. Front Cell Dev Biol 8 120 (2020)
  7. Peptidyl-prolyl isomerases: functionality and potential therapeutic targets in cardiovascular disease. Rostam MA, Piva TJ, Rezaei HB, Kamato D, Little PJ, Zheng W, Osman N. Clin Exp Pharmacol Physiol 42 117-124 (2015)
  8. Gears-In-Motion: The Interplay of WW and PPIase Domains in Pin1. Lee YM, Liou YC. Front Oncol 8 469 (2018)
  9. Polyubiquitination inhibition of estrogen receptor alpha and its implications in breast cancer. Tecalco-Cruz AC, Ramírez-Jarquín JO. World J Clin Oncol 9 60-70 (2018)
  10. Roles of peptidyl-prolyl isomerase Pin1 in disease pathogenesis. Li J, Mo C, Guo Y, Zhang B, Feng X, Si Q, Wu X, Zhao Z, Gong L, He D, Shao J. Theranostics 11 3348-3358 (2021)
  11. Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy. Chuang HH, Zhen YY, Tsai YC, Chuang CH, Huang MS, Hsiao M, Yang CJ. Biomedicines 9 359 (2021)

Articles citing this publication (31)



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