Literature DB >> 31175010

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

Fleur M Ferguson1, Zainab M Doctor1, Scott B Ficarro2, Jarrod A Marto3, Nam Doo Kim4, Taebo Sim5, Nathanael S Gray6.   

Abstract

The TAIRE family of kinases are an understudied branch of the CDK kinase family, that have been implicated in a number of cancers. This manuscript describes the design, synthesis and SAR of covalent CDK14 inhibitors, culminating in identification of FMF-04-159-2, a potent, covalent CDK14 inhibitor with a TAIRE kinase biased selectivity profile.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  CDK inhibitor; CDK14; CDK15; CDK16; CDK17; CDK18; Cell cycle; Covalent kinase inhibitor; Mitosis; TAIRE kinase

Mesh：

Substances：

Year:  2019        PMID： 31175010      PMCID： PMC6886737          DOI： 10.1016/j.bmcl.2019.05.024

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


  15 in total

1.  Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity.

Authors:  Fleur M Ferguson; Zainab M Doctor; Scott B Ficarro; Christopher M Browne; Jarrod A Marto; Jared L Johnson; Tomer M Yaron; Lewis C Cantley; Nam Doo Kim; Taebo Sim; Matthew J Berberich; Marian Kalocsay; Peter K Sorger; Nathanael S Gray
Journal:  Cell Chem Biol       Date:  2019-03-28       Impact factor: 8.116

Review 2.  The Cysteinome of Protein Kinases as a Target in Drug Development.

Authors:  Apirat Chaikuad; Pierre Koch; Stefan A Laufer; Stefan Knapp
Journal:  Angew Chem Int Ed Engl       Date:  2018-02-02       Impact factor: 15.336

3.  In situ kinase profiling reveals functionally relevant properties of native kinases.

Authors:  Matthew P Patricelli; Tyzoon K Nomanbhoy; Jiangyue Wu; Heidi Brown; David Zhou; Jianming Zhang; Subadhra Jagannathan; Arwin Aban; Eric Okerberg; Chris Herring; Brian Nordin; Helge Weissig; Qingkai Yang; Jiing-Dwan Lee; Nathanael S Gray; John W Kozarich
Journal:  Chem Biol       Date:  2011-06-24

4.  Cell cycle control of wnt receptor activation.

Authors:  Gary Davidson; Jinlong Shen; Ya-Lin Huang; Yi Su; Emil Karaulanov; Kerstin Bartscherer; Christine Hassler; Peter Stannek; Michael Boutros; Christof Niehrs
Journal:  Dev Cell       Date:  2009-12       Impact factor: 12.270

5.  PFTK1 regulates cell proliferation, migration and invasion in epithelial ovarian cancer.

Authors:  Weiwei Zhang; Rong Liu; Chunhui Tang; Qinghua Xi; Shumin Lu; Wenjuan Chen; Lianxin Zhu; Jialin Cheng; Yannan Chen; Wei Wang; Jianxin Zhong; Yan Deng
Journal:  Int J Biol Macromol       Date:  2016-01-06       Impact factor: 6.953

6.  Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.

Authors:  Paul G Wyatt; Andrew J Woodhead; Valerio Berdini; John A Boulstridge; Maria G Carr; David M Cross; Deborah J Davis; Lindsay A Devine; Theresa R Early; Ruth E Feltell; E Jonathan Lewis; Rachel L McMenamin; Eva F Navarro; Michael A O'Brien; Marc O'Reilly; Matthias Reule; Gordon Saxty; Lisa C A Seavers; Donna-Michelle Smith; Matt S Squires; Gary Trewartha; Margaret T Walker; Alison J-A Woolford
Journal:  J Med Chem       Date:  2008-07-26       Impact factor: 7.446

Review 7.  The kinome 'at large' in cancer.

Authors:  Emmy D G Fleuren; Luxi Zhang; Jianmin Wu; Roger J Daly
Journal:  Nat Rev Cancer       Date:  2016-02       Impact factor: 60.716

8.  PFTK1 Promotes Gastric Cancer Progression by Regulating Proliferation, Migration and Invasion.

Authors:  Lei Yang; Jia Zhu; Hua Huang; Qichang Yang; Jing Cai; Qiuhong Wang; Junya Zhu; Mengting Shao; Jinzhang Xiao; Jie Cao; Xiaodan Gu; Shusen Zhang; Yingying Wang
Journal:  PLoS One       Date:  2015-10-21       Impact factor: 3.240

Review 9.  Cyclin-dependent kinases.

Authors:  Marcos Malumbres
Journal:  Genome Biol       Date:  2014       Impact factor: 13.583

10.  The structure and substrate specificity of human Cdk12/Cyclin K.

Authors:  Christian A Bösken; Lucas Farnung; Corinna Hintermair; Miriam Merzel Schachter; Karin Vogel-Bachmayr; Dalibor Blazek; Kanchan Anand; Robert P Fisher; Dirk Eick; Matthias Geyer
Journal:  Nat Commun       Date:  2014-03-24       Impact factor: 14.919
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  1 in total

Review 1.  Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011-2020): Current Status and Future Prospects.

Authors:  Mohammed I El-Gamal; Seyed-Omar Zaraei; Moustafa M Madkour; Hanan S Anbar
Journal:  Molecules       Date:  2022-01-05       Impact factor: 4.411
  1 in total

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