The design strategy of selective PTP1B inhibitors over TCPTP |
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| Affiliation: | 1. School of Life Science and Biotechnology, Dalian University of Technology, Dalian 116024, Liaoning, China;2. New Drug Research and Development Center, North China Pharmaceutical Group Corporation, National Microbial Medicine Engineering and Research Center, Shijiazhuang 050015, China;3. Research Center for Marine Drugs, School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China;4. Key Laboratory of Biotechnology and Bioresources Utilization, Dalian Minzu University, Dalian 116024, Liaoning, China |
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| Abstract: | Protein tyrosine phosphatase 1B (PTP1B) has already been well studied as a highly validated therapeutic target for diabetes and obesity. However, the lack of selectivity limited further studies and clinical applications of PTP1B inhibitors, especially over T-cell protein tyrosine phosphatase (TCPTP). In this review, we enumerate the published specific inhibitors of PTP1B, discuss the structure–activity relationships by analysis of their X-ray structures or docking results, and summarize the characteristic of selectivity related residues and groups. Furthermore, the design strategy of selective PTP1B inhibitors over TCPTP is also proposed. We hope our work could provide an effective way to gain specific PTP1B inhibitors. |
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| Keywords: | Selectivity PTP1B inhibitor TCPTP Diabetes Design strategy |
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