Recent advance on PTP1B inhibitors and their biomedical applications

Bigyan Sharma, Liuxing Xie, Fen Yang, Wei Wang, Quanming Zhou, Menghua Xiang, Shizhe Zhou, Wanting Lv, Yan Jia, Laxman Pokhrel, Jun Shen, Qicai Xiao, Liqian Gao, Wenbin Deng

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

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.

Original languageEnglish (US)
Article number112376
JournalEuropean Journal of Medicinal Chemistry
Volume199
DOIs
StatePublished - Aug 1 2020
Externally publishedYes

Keywords

  • Bidentate
  • High-throughput screening
  • Inhibitor
  • PTP1B

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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