High-Throughput Discovery and Characterization of Covalent Inhibitors for Protein Tyrosine Phosphatases.
Methods in molecular biology (Clifton, N.J.)(2024)
摘要
Covalent inhibition has gained increasing interest in targeting the undruggable protein tyrosine phosphatases (PTPs). However, a systematic method for discovering and characterizing covalent PTP inhibitors has yet to be established. Here, we describe a workflow involving high-throughput screening of covalent fragment libraries and a novel biochemical assay that enables the acquisition of kinetics parameters of PTP inhibition by covalent inhibitors with higher throughput.
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