作者:Leandro Piovan、Li Wu、Zhong-Yin Zhang、Leandro H. Andrade
DOI:10.1039/c0ob01050b
日期:——
A series of organochalcogenanes was synthesized and evaluated as proteintyrosine phosphatases (PTPs) inhibitors. The results indicate that organochalcogenanes inactivate the PTPs in a time- and concentration-dependent fashion, most likely through covalent modification of the active site sulfur-moiety by the chalcogen atom. Consequently, organochalcogenanes represent a new class of mechanism-based probes to modulate the PTP-mediated cellular processes.
研究人员合成了一系列有机卤化烷,并将其作为酪氨酸蛋白磷酸酶(PTPs)抑制剂进行了评估。结果表明,有机钙原烷以时间和浓度依赖性的方式使 PTPs 失活,这很可能是通过钙原原子对活性位点硫基的共价修饰实现的。因此,有机钙原烷代表了一类基于机制的新型探针,可用于调节 PTP 介导的细胞过程。