PTP1B as a drug target

recent developments in PTP1B inhibitor discovery

Sheng Zhang, Zhong-Yin Zhang

Research output: Contribution to journalArticle

399 Citations (Scopus)

Abstract

Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of both type 2 diabetes and obesity; however, targeting PTP1B for drug discovery is challenging because of the highly conserved and positively charged active-site pocket. Tremendous progress has been made in the development of potent and selective PTP1B inhibitors that engage both the active site and no catalytic sites. Several strategies are being pursued to improve the pharmacological properties of PTP1B inhibitors. These new developments suggest that it is feasible to acquire PTP1B-based, small-molecule therapeutics with the requisite potency and selectivity. Future efforts will probably transform the potent and selective PTP1B inhibitors into orally available drugs with desirable physicochemical properties and in vivo efficacies.

Original languageEnglish
Pages (from-to)373-381
Number of pages9
JournalDrug Discovery Today
Volume12
Issue number9-10
DOIs
StatePublished - May 2007

Fingerprint

Non-Receptor Type 1 Protein Tyrosine Phosphatase
Pharmaceutical Preparations
Catalytic Domain
Drug Discovery
Type 2 Diabetes Mellitus
Obesity
Pharmacology

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

PTP1B as a drug target : recent developments in PTP1B inhibitor discovery. / Zhang, Sheng; Zhang, Zhong-Yin.

In: Drug Discovery Today, Vol. 12, No. 9-10, 05.2007, p. 373-381.

Research output: Contribution to journalArticle

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