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Issue 1, 2018
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In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases

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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.

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

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Publication details

The article was received on 09 Oct 2017, accepted on 01 Nov 2017 and first published on 08 Dec 2017


Article type: Review Article
DOI: 10.1039/C7MD00510E
Citation: Med. Chem. Commun., 2018,9, 44-66
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    In depth analysis of kinase cross screening data to identify chemical starting points for inhibition of the Nek family of kinases

    C. I. Wells, N. R. Kapadia, R. M. Couñago and D. H. Drewry, Med. Chem. Commun., 2018, 9, 44
    DOI: 10.1039/C7MD00510E

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