高通量发现和鉴定蛋白质酪氨酸磷酸酶的共价抑制剂。
High-Throughput Discovery and Characterization of Covalent Inhibitors for Protein Tyrosine Phosphatases.
机构信息
Department of Chemistry, Purdue University, West Lafayette, IN, USA.
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, USA.
出版信息
Methods Mol Biol. 2024;2743:301-316. doi: 10.1007/978-1-0716-3569-8_19.
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.
共价抑制在靶向不可成药的蛋白酪氨酸磷酸酶（PTPs）方面引起了越来越多的关注。然而，一种系统的发现和表征共价 PTP 抑制剂的方法尚未建立。在这里，我们描述了一种涉及高通量筛选共价片段文库和一种新的生化测定的工作流程，该方法能够以更高的通量获得共价抑制剂对 PTP 抑制的动力学参数。
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