2. Academic Validation
  3. Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships

Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships

  • Bioorg Med Chem Lett. 2017 Aug 1;27(15):3382-3385. doi: 10.1016/j.bmcl.2017.06.001.
Wenlong Sun 1,  Chunlin Zhuang 2,  Xia Li 1,  Bowei Zhang 1,  Xinhua Lu 3,  Zhihui Zheng 4,  Yuesheng Dong 5
Affiliations

Affiliations

  • 1 School of Life Science, Biotechnology, Dalian University of Technology, Dalian, Liaoning 116024, China.
  • 2 School of Pharmacy, Second Military Medical University, 325 Guohe Road, Shanghai 200433, China. Electronic address: zclnathan@163.com.
  • 3 New Drug Research and Development Center, North China Pharmaceutical Group Corporation and National Microbial Medicine Engineering and Research Center, Shijiazhuang, Hebei 050015, China. Electronic address: luxinhua89@yeah.net.
  • 4 New Drug Research and Development Center, North China Pharmaceutical Group Corporation and National Microbial Medicine Engineering and Research Center, Shijiazhuang, Hebei 050015, China.
  • 5 School of Life Science, Biotechnology, Dalian University of Technology, Dalian, Liaoning 116024, China. Electronic address: yshdong@dlut.edu.cn.
PMID: 28642102 DOI: 10.1016/j.bmcl.2017.06.001
Abstract

Protein tyrosine Phosphatase 1B (PTP1B) inhibitors as potential therapies for diabetes and obesity have attracted much attention in recent years. Six varic acid analogues were isolated from two strains of fungi and evaluated for PTP1B inhibition activities. The structure-activity relationships were also characterized and predicted by molecular modeling. Further kinetic studies indicated the reversible and competitive inhibition manner of varic acid analogues. Trivaric acid showed insulin-sensitizing effect not only in vitro but also in vivo, representing a promising lead compound for further optimization.

Keywords

Insulin-sensitizing effect; PTP1B; Structure–activity relationships; Type 2 diabetes mellitus; Varic acid.

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