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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