Abstract
We have successfully designed and assembled a 66-member library of protein tyrosine phosphatases (PTP) inhibitor candidates using α-ketoacid-hydroxylamine (KAHA) ligation. Subsequent in situ enzymatic screening revealed a potent hit (IC50=1.67μM) against PTP1B, which displayed 6.8- to 50-fold selectivity over other phosphatases.
Published Version
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