Targeted Degradation of the Aryl Hydrocarbon Receptor by the PROTAC Approach: A Useful Chemical Genetic Tool

Abstract

License to degrade. A chimeric small molecule or PROTAC (PROteolysis TArgeting Chimera) based on the chemopreventive natural product apigenin was developed (see scheme). The molecule was shown to target the aryl hydrocarbon receptor (AHR) for degradation by the proteasome.

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