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Proximity-enabled bioreactivity to generate covalent peptide inhibitors of p53-Mdm4
1Department of Pharmaceutical Chemistry and the Cardiovascular Research Institute, University of California, San Francisco, 555 Mission Bay Blvd South, San Francisco, CA 94158, USA. Lei.Wang2@ucsf.edu.
Chemical Communications (Cambridge, England)
|March 22, 2016
Abstract:
Although small molecule covalent inhibitors have been widely explored, macromolecular covalent inhibitors are more difficult to design and implement. Here we present a strategy to enable a peptide to bind to its target protein covalently via proximity-enabled bioreactivity, improving its activity of inhibiting the p53-Mdm4 interaction by 10-fold.
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