Expanding the Opportunities for Modulating Kinase Targets with Allosteric Approaches

Author(s): Henrik Mobitz, Wolfgang Jahnke, Sandra W. Cowan-Jacob

Journal Name: Current Topics in Medicinal Chemistry

Volume 17 , Issue 1 , 2017

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Graphical Abstract:


The need for novel approaches for targeting well-known protein families in drug discovery has been discussed for several years. There is a huge amount of literature on the inhibition of kinases with small molecules targeting the ATP site, and as a result of this extensive research, there are a large number of kinase inhibitors in the clinic. However, even though the idea of targeting other sites on kinases is not new, relatively little has been reported. In this review we give an overview of structurally characterized allosteric kinase inhibitors, outline the benefits of these with the use of case studies and then discuss the challenges that need to be overcome and the opportunities for doing this.

Keywords: Activator, Allosteric, Binding mode, Inhibitor, Kinase, Structure-Based Drug Discovery, Target Space.

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Article Details

Year: 2017
Published on: 13 November, 2016
Page: [59 - 70]
Pages: 12
DOI: 10.2174/1568026616666160719165314
Price: $65

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