Abstract
AbstractDemand for peptide‐based pharmaceuticals has been steadily increasing, but only limited success has been achieved to date. To expedite peptide‐based drug discovery, we developed a general scheme for cell‐based screening of cyclic peptide inhibitors armed with a user‐designed warhead. We combined unnatural amino acid incorporation and split intein‐mediated peptide cyclization techniques and integrated a yeast‐based colorimetric screening assay to generate a new scheme that we call the custom‐designed warhead‐armed cyclic peptide screening platform (CWCPS). This strategy successfully discovered a potent inhibitor, CY5‐6Q, that targets human histone deacetylase 8 (HDAC8) with a KD value of 15 nM. This approach can be a versatile and general platform for discovering cyclic peptide inhibitors.
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