Related Experiment Video
Updated: Jul 7, 2025
Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
Published on: June 30, 2019
High-Throughput Discovery and Characterization of Covalent Inhibitors for Protein Tyrosine Phosphatases
Zihan Qu1, Aaron D Krabill2, Zhong-Yin Zhang3,4,5,6
1Department of Chemistry, Purdue University, West Lafayette, IN, USA.
Abstract:
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.
