Exploring the roles of protein kinases using chemical genetics

Authors: Elphick, Lucy M; Lee, Sarah E; Anderson, Alexandra A; Child, Emma S; Bonnac, Laurent; Gouverneur, Véronique; Mann, David J

Source: Future Medicinal Chemistry, Volume 1, Number 7, October 2009 , pp. 1233-1241(9)

Publisher: Future Science

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Abstract:

The protein kinase superfamily is one of the most important families of enzymes in molecular biology. Protein kinases typically catalyze the transfer of the γ-phosphate from ATP to a protein substrate (a highly ubiquitous cellular reaction), thereby controlling key areas of cell regulation. Deregulation of protein kinases is known to contribute to many human diseases, and selective inhibitors of protein kinases are a major area of interest in medicinal chemistry. However, a detailed understanding of many kinase pathways is currently lacking. Before we can effectively design medicinally relevant selective kinase inhibitors, it is necessary to understand the role played by a given kinase in specific signal-transduction cascades and to decipher its protein targets. Here, we describe recent advances towards dissecting protein kinase function through the use of chemical genetics.

Document Type: Research article

DOI: http://dx.doi.org/10.4155/fmc.09.50

Affiliations: 1: 1Division of Cell & Molecular Biology, Imperial College London, SW7 2AZ, UK., Email: d.mann@imperial.ac.uk

Publication date: 2009-10-01

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Future Medicinal Chemistry delivers expert commentary and analysis on emerging research toward the establishment of new medicines - from the identification of targets, through to the synthesis and evaluation of putative therapeutic entities.
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