Issue 1, 2018

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

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

Supplementary files

Article information

Article type
Review Article
Submitted
09 Oct 2017
Accepted
01 Nov 2017
First published
08 Dec 2017

Med. Chem. Commun., 2018,9, 44-66

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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