ChemBioChem · 2007 · 93 citations · 20 references
Bioorganic ChemistryMolecular BiologyChemical BiologyEnzymatic ModificationBiochemical GeneticsProtein DegradationBiotransformationBiochemistryG Protein-coupled ReceptorAryl Hydrocarbon ReceptorReceptor (Biochemistry)Mechanism Of ActionDrug DevelopmentProteolysis Targeting ChimeraPharmacologyNatural SciencesDrug DiscoveryMedicineChimeric Small MoleculeCarbonyl MetabolismProtac Approach
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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