Literature DB >> 20932746

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

Andrew Potter1, Victoria Oldfield, Claire Nunns, Christophe Fromont, Stuart Ray, Christopher J Northfield, Christopher J Bryant, Simon F Scrace, David Robinson, Natalia Matossova, Lisa Baker, Pawel Dokurno, Allan E Surgenor, Ben Davis, Christine M Richardson, James B Murray, Jonathan D Moore.   

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.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20932746     DOI: 10.1016/j.bmcl.2010.09.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  21 in total

1.  Prolyl isomerase Pin1 negatively regulates AMP-activated protein kinase (AMPK) by associating with the CBS domain in the γ subunit.

Authors:  Yusuke Nakatsu; Misaki Iwashita; Hideyuki Sakoda; Hiraku Ono; Kengo Nagata; Yasuka Matsunaga; Toshiaki Fukushima; Midori Fujishiro; Akifumi Kushiyama; Hideaki Kamata; Shin-Ichiro Takahashi; Hideki Katagiri; Hiroaki Honda; Hiroshi Kiyonari; Takafumi Uchida; Tomoichiro Asano
Journal:  J Biol Chem       Date:  2015-08-14       Impact factor: 5.157

2.  Prolyl isomerase Pin1 acts downstream of miR200c to promote cancer stem-like cell traits in breast cancer.

Authors:  Man-Li Luo; Chang Gong; Chun-Hau Chen; Daniel Y Lee; Hai Hu; Pengyu Huang; Yandan Yao; Wenjun Guo; Ferenc Reinhardt; Gerburg Wulf; Judy Lieberman; Xiao Zhen Zhou; Erwei Song; Kun Ping Lu
Journal:  Cancer Res       Date:  2014-05-01       Impact factor: 12.701

Review 3.  Peptidyl-Proline Isomerases (PPIases): Targets for Natural Products and Natural Product-Inspired Compounds.

Authors:  Bryan M Dunyak; Jason E Gestwicki
Journal:  J Med Chem       Date:  2016-07-25       Impact factor: 7.446

4.  Neighboring phosphoSer-Pro motifs in the undefined domain of IRAK1 impart bivalent advantage for Pin1 binding.

Authors:  Monique J Rogals; Alexander I Greenwood; Jeahoo Kwon; Kun Ping Lu; Linda K Nicholson
Journal:  FEBS J       Date:  2016-11-20       Impact factor: 5.542

5.  A Phosphoramidate Strategy Enables Membrane Permeability of a Non-nucleotide Inhibitor of the Prolyl Isomerase Pin1.

Authors:  Daniel M C Schwarz; Sarah K Williams; Maxwell Dillenburg; Carston R Wagner; Jason E Gestwicki
Journal:  ACS Med Chem Lett       Date:  2020-08-10       Impact factor: 4.345

6.  Regioselective Synthesis of 2-Aryl-5-cyano-1-(2-hydroxyaryl)-1H-imidazole-4-carboxamides Self-Assisted by a 2-Hydroxyaryl Group.

Authors:  Fábio Pedroso de Lima; Emilio Lence; Pilar Suárez de Cepeda; Carla Correia; M Alice Carvalho; Concepción González-Bello; M Fernanda Proença
Journal:  ACS Omega       Date:  2022-06-24

Review 7.  The isomerase PIN1 controls numerous cancer-driving pathways and is a unique drug target.

Authors:  Xiao Zhen Zhou; Kun Ping Lu
Journal:  Nat Rev Cancer       Date:  2016-06-03       Impact factor: 60.716

8.  DeepFrag: An Open-Source Browser App for Deep-Learning Lead Optimization.

Authors:  Harrison Green; Jacob D Durrant
Journal:  J Chem Inf Model       Date:  2021-05-24       Impact factor: 4.956

Review 9.  Roles of Prolyl Isomerases in RNA-Mediated Gene Expression.

Authors:  Roopa Thapar
Journal:  Biomolecules       Date:  2015-05-18

10.  DeepFrag: a deep convolutional neural network for fragment-based lead optimization.

Authors:  Harrison Green; David R Koes; Jacob D Durrant
Journal:  Chem Sci       Date:  2021-05-08       Impact factor: 9.825

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