Literature DB >> 30108900

In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases.

C I Wells1, N R Kapadia1, R M Couñago2, D H Drewry1.   

Abstract

Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function can also then serve as chemical starting points in these drug discovery efforts. The Nek family of kinases has received very little attention, as judged by number of citations in PubMed, yet they appear to play many key roles and have been implicated in disease. Here we present our work to identify high quality chemical starting points that have emerged due to the increased incidence of broad kinome screening. We anticipate that this analysis will allow the community to progress towards the generation of chemical probes and eventually drugs that target members of the Nek family.

Year:  2017        PMID: 30108900      PMCID: PMC6071746          DOI: 10.1039/c7md00510e

Source DB:  PubMed          Journal:  Medchemcomm        ISSN: 2040-2503            Impact factor:   3.597


  113 in total

1.  Cloning and characterization of the murine Nek3 protein kinase, a novel member of the NIMA family of putative cell cycle regulators.

Authors:  K Tanaka; E A Nigg
Journal:  J Biol Chem       Date:  1999-05-07       Impact factor: 5.157

2.  NEK1 and DYNC2H1 are both involved in short rib polydactyly Majewski type but not in Beemer Langer cases.

Authors:  Joyce El Hokayem; Céline Huber; Adeline Couvé; Jacqueline Aziza; Geneviève Baujat; Raymonde Bouvier; Denise P Cavalcanti; Felicity A Collins; Marie-Pierre Cordier; Anne-Lise Delezoide; Marie Gonzales; Diana Johnson; Martine Le Merrer; Annie Levy-Mozziconacci; Philippe Loget; Dominique Martin-Coignard; Jelena Martinovic; Geert R Mortier; Marie-José Perez; Joëlle Roume; Gioacchino Scarano; Arnold Munnich; Valérie Cormier-Daire
Journal:  J Med Genet       Date:  2012-04       Impact factor: 6.318

3.  The NIMA-family kinase Nek3 regulates microtubule acetylation in neurons.

Authors:  Jufang Chang; Robert H Baloh; Jeffrey Milbrandt
Journal:  J Cell Sci       Date:  2009-06-09       Impact factor: 5.285

Review 4.  FDA-approved small-molecule kinase inhibitors.

Authors:  Peng Wu; Thomas E Nielsen; Mads H Clausen
Journal:  Trends Pharmacol Sci       Date:  2015-05-12       Impact factor: 14.819

5.  Purification, cloning, and characterization of Nek8, a novel NIMA-related kinase, and its candidate substrate Bicd2.

Authors:  Pamela M Holland; Alison Milne; Kirsten Garka; Richard S Johnson; Cynthia Willis; John E Sims; Charles T Rauch; Timothy A Bird; G Duke Virca
Journal:  J Biol Chem       Date:  2002-02-25       Impact factor: 5.157

6.  Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities.

Authors:  Jian-Bei Xi; Yan-Fen Fang; Brendan Frett; Meng-Li Zhu; Tong Zhu; Yan-Nan Kong; Feng-Jie Guan; Yun Zhao; Xiong-Wen Zhang; Hong-Yu Li; Ming-Liang Ma; Wenhao Hu
Journal:  Eur J Med Chem       Date:  2016-12-12       Impact factor: 6.514

7.  NIMA-related protein kinase 1 is involved early in the ionizing radiation-induced DNA damage response.

Authors:  Rosaria Polci; Aimin Peng; Phang-Lang Chen; Daniel J Riley; Yumay Chen
Journal:  Cancer Res       Date:  2004-12-15       Impact factor: 12.701

8.  Selectivity-determining residues in Plk1.

Authors:  Michael Kothe; Darcy Kohls; Simon Low; Rocco Coli; Glen R Rennie; Frederic Feru; Cyrille Kuhn; Yuan-Hua Ding
Journal:  Chem Biol Drug Des       Date:  2007-11-13       Impact factor: 2.817

9.  Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression.

Authors:  John E Bisi; Jessica A Sorrentino; Patrick J Roberts; Francis X Tavares; Jay C Strum
Journal:  Mol Cancer Ther       Date:  2016-01-29       Impact factor: 6.261

10.  The NIMA-family kinase, Nek1 affects the stability of centrosomes and ciliogenesis.

Authors:  Mark C White; Lynne M Quarmby
Journal:  BMC Cell Biol       Date:  2008-06-04       Impact factor: 4.241

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  8 in total

1.  Crowdsourced mapping of unexplored target space of kinase inhibitors.

Authors:  Anna Cichońska; Balaguru Ravikumar; Robert J Allaway; Fangping Wan; Sungjoon Park; Olexandr Isayev; Shuya Li; Michael Mason; Andrew Lamb; Ziaurrehman Tanoli; Minji Jeon; Sunkyu Kim; Mariya Popova; Stephen Capuzzi; Jianyang Zeng; Kristen Dang; Gregory Koytiger; Jaewoo Kang; Carrow I Wells; Timothy M Willson; Tudor I Oprea; Avner Schlessinger; David H Drewry; Gustavo Stolovitzky; Krister Wennerberg; Justin Guinney; Tero Aittokallio
Journal:  Nat Commun       Date:  2021-06-03       Impact factor: 14.919

2.  Structure-Activity Relationship (SAR) Study of Spautin-1 to Entail the Discovery of Novel NEK4 Inhibitors.

Authors:  Mathias Elsocht; Philippe Giron; Laila Maes; Wim Versées; Gustavo J Gutierrez; Jacques De Grève; Steven Ballet
Journal:  Int J Mol Sci       Date:  2021-01-10       Impact factor: 5.923

3.  Temozolomide-induced guanine mutations create exploitable vulnerabilities of guanine-rich DNA and RNA regions in drug-resistant gliomas.

Authors:  Deanna M Tiek; Beril Erdogdu; Roham Razaghi; Lu Jin; Norah Sadowski; Carla Alamillo-Ferrer; J Robert Hogg; Bassem R Haddad; David H Drewry; Carrow I Wells; Julie E Pickett; Xiao Song; Anshika Goenka; Bo Hu; Samuel A Goldlust; William J Zuercher; Mihaela Pertea; Winston Timp; Shi-Yuan Cheng; Rebecca B Riggins
Journal:  Sci Adv       Date:  2022-06-22       Impact factor: 14.957

4.  Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine.

Authors:  Matthew J Byrne; Nazia Nasir; Christine Basmadjian; Chitra Bhatia; Rory F Cunnison; Katherine H Carr; Corine Mas-Droux; Sharon Yeoh; Céline Cano; Richard Bayliss
Journal:  Biochem J       Date:  2020-04-30       Impact factor: 3.857

Review 5.  Checking NEKs: Overcoming a Bottleneck in Human Diseases.

Authors:  Andressa Peres de Oliveira; Luidy Kazuo Issayama; Isadora Carolina Betim Pavan; Fernando Riback Silva; Talita Diniz Melo-Hanchuk; Fernando Moreira Simabuco; Jörg Kobarg
Journal:  Molecules       Date:  2020-04-13       Impact factor: 4.411

6.  Identification and antitumor activity of a novel inhibitor of the NIMA-related kinase NEK6.

Authors:  Marta De Donato; Benedetta Righino; Flavia Filippetti; Alessandra Battaglia; Marco Petrillo; Davide Pirolli; Giovanni Scambia; Maria Cristina De Rosa; Daniela Gallo
Journal:  Sci Rep       Date:  2018-10-30       Impact factor: 4.379

7.  Plasmodial Kinase Inhibitors: License to Cure?

Authors:  Diego González Cabrera; André Horatscheck; Colin R Wilson; Greg Basarab; Charles J Eyermann; Kelly Chibale
Journal:  J Med Chem       Date:  2018-06-04       Impact factor: 7.446

8.  Expression of the NEK family in normal and cancer tissue: an immunohistochemical study.

Authors:  Talita Diniz Melo-Hanchuk; Mariana Bonjiorno Martins; Lucas Leite Cunha; Fernando Augusto Soares; Laura Sterian Ward; José Vassallo; Jörg Kobarg
Journal:  BMC Cancer       Date:  2020-01-06       Impact factor: 4.430

  8 in total

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