Biomedical Laboratory Science

ShareThis

Showing posts with label Mutant. Show all posts
Showing posts with label Mutant. Show all posts

Monday, August 8, 2016

Literature Review: Targeting Mutant Kinases

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.


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]
Source: genengnews
Related Posts Plugin for WordPress, Blogger...

AddToAny