Small-Molecule Kinase Inhibitors Have Typically Been Designed To Inhibit Wild-Type Kinases Rather Than the Mutant Forms
Kinases have been the target of extensive research to identify drugs to treat a variety of diseases in which the wild-type kinase or a mutant kinase plays a crucial role. Kinase mutations frequently lead to an activated state where the kinase is always active and no longer tightly regulated. Considering resistance mutations are also important for kinase inhibitors. A frequent escape route is a mutation to the gatekeeper amino acid that blocks inhibitor binding. A variety of large screening panels have been developed that range from binding assays to enzyme assays, each with their unique pros and cons.
Read more: Literature Review: Targeting Mutant Kinases
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A variety of large screening panels have been developed that range from binding assays
to enzyme assays, each with their unique pros and cons. [nicolas_/Getty]
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Source: genengnews
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