Recent advance on PTP1B inhibitors and their biomedical applications

Eur J Med Chem. 2020 Aug 1:199:112376. doi: 10.1016/j.ejmech.2020.112376. Epub 2020 May 6.

Abstract

Protein Tyrosine Phosphatase 1B (PTP1B), as one of the most important members in PTP superfamily, plays a vital role in conducting various cellular functions. So far, PTP1B has been reported to be involved in the development of many diseases including obesity, diabetes, cancers and cardiovascular diseases. Development of potent and specific PTP1B inhibitors and studies on the structure-activity relationship (SAR) between their chemical structures and their biological activity have drawn increasing attention as they could not only modulate the PTP1B functions inside the cells but also provide useful lead compounds for the treatment of various PTP1B-associated diseases. To this end, we herein summarized the recent developments of PTP1B inhibitors, and different kinds of high-throughput screening strategies for the identification of potential PTP1B inhibitors as well as their potential biomedical applications, and we also provided some perspectives in the concluding remarks in this work.

Keywords: Bidentate; High-throughput screening; Inhibitor; PTP1B.

Publication types

  • Review

MeSH terms

  • Biomedical Research*
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism

Substances

  • Coordination Complexes
  • Enzyme Inhibitors
  • PTPN1 protein, human
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1