Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors.
作者： Renshuai Zhang , Rilei Yu , Qi Xu , Xiangqian Li , Jiao Luo
DOI: 10.1016/J.EJMECH.2017.04.004
关键词:
摘要: Protein tyrosine phosphatase 1B (PTP1B) is a key negative regulator of insulin signaling pathway. Inhibition PTP1B expected to improve action. Appropriate selectivity and permeability are the gold standard for excellent inhibitors. In this work, molecular hybridization-based screening identified selective competitive inhibitor. Compound 10a has IC50 values 199 nM against PTP1B, shows 32-fold over closely related TCPTP. Molecule docking dynamics studies reveal reason Moreover, cell cellular activity compound demonstrated respectively.
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