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Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of both insulin and leptin signals. For years, inhibiting of PTP1B has been considered to be a potential therapeutics for treating Type 2 diabetes and obesity. Recently, we recognized lithocholic acid (LCA) as a natural inhibitor against PTP1B (IC(50)=12.74 μM) by a vertical screen for the first time. Further SAR research was carried out by synthesizing and evaluating a series of compounds bearing two methyls at C-4 position and a fused heterocycle to ring A. Among them, compound 14b achieved a PTP1B inhibitory activity about eightfold than LCA and a 14-fold selectivity over the homogenous enzyme TCPTP. Copyright © 2012 Elsevier Ltd. All rights reserved.


Hai-Bing He, Li-Xin Gao, Qi-Feng Deng, Wei-Ping Ma, Chun-Lan Tang, Wen-Wei Qiu, Jie Tang, Jing-Ya Li, Jia Li, Fan Yang. Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B. Bioorganic & medicinal chemistry letters. 2012 Dec 1;22(23):7237-42

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PMID: 23067554

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