Target validation: Switching domains

August 18th, 2016 by Alessio Ciulli

Nature Chemical Biology 12, 659 (2016). doi:10.1038/nchembio.2154

Author: Alessio Ciulli

Chemical probes and drugs often bind to functional domains on disease-relevant proteins. A study suggests a chemical genetic approach to establish on-target effects by swapping the targeted domain, affording resistance to pharmacological inhibition while retaining functionality.