Peptidomimetics as potent and selective PTP1B inhibitors

Med Chem. 2013 Aug;9(5):660-71. doi: 10.2174/1573406411309050005.

Abstract

A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms discovery of highly potent and selective PTP1B inhibitors.

MeSH terms

  • Acetates / chemistry
  • Amides / chemistry
  • Dipeptides / chemistry
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Peptidomimetics*
  • Piperidines / chemistry
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Acetates
  • Amides
  • Dipeptides
  • Enzyme Inhibitors
  • Peptidomimetics
  • Piperidines
  • piperidine
  • PTPN1 protein, human
  • Protein Tyrosine Phosphatase, Non-Receptor Type 1