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The 10 things you should know about protein kinases and inhibitors

Fabbro, Doriano and Jacob, Sandra and Moebitz, Henrik (2015) The 10 things you should know about protein kinases and inhibitors. British Journal of Pharmacology, 172 (11). pp. 2675-2700. ISSN 00071188

Abstract

Many human malignancies are associated with deregulated activation of protein or lipid kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein and lipid kinases, therefore, represent, after GPCRs and proteases an important target classes for treating human disorders. This review focus on “the 10 things you should know about protein kinases and their inhibitors” including a short introduction on the history on protein kinases and inhibitor and ending with a perspective in kinase drug discovery. Although the “10 things” have been, to a certain extent, chosen arbitrarily, they cover in a comprehensive way the past and present efforts in kinase drug discovery and summarize the “status quo” of the current kinase inhibitors as well as knowledge about kinase structure and binding modes. Besides describing the potentials of protein kinase inhibitors as drugs this review also focus on their limitations, in particular on how to circumvent emerging resistance against kinase inhibitors in oncological indications.

Item Type: Article
Date Deposited: 14 Jun 2016 23:45
Last Modified: 14 Jun 2016 23:45
URI: https://oak.novartis.com/id/eprint/23619

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