Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3561-4. doi: 10.1016/j.bmcl.2013.04.031. Epub 2013 Apr 23.

Abstract

Probestin is a potent aminopeptidase N (APN) inhibitor originally isolated from the bacterial culture broth. Here, we report probestin synthesis by solid phase peptide synthesis (SPPS) method and evaluated its activity to inhibit angiogenesis using a chicken embryo chorioallantoic membrane (CAM) assay and a CAM tumor xenograft model. Results from these studies demonstrate that probestin inhibits the angiogenic activity and tumor growth.

Publication types

  • Letter
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis*
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Breast Neoplasms / blood supply
  • Breast Neoplasms / drug therapy
  • CD13 Antigens / antagonists & inhibitors
  • Cell Line, Tumor
  • Chick Embryo
  • Chorioallantoic Membrane / blood supply
  • Female
  • Humans
  • Mice, Inbred BALB C
  • Neovascularization, Physiologic / drug effects
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*
  • Solid-Phase Synthesis Techniques / methods
  • Xenograft Model Antitumor Assays

Substances

  • Angiogenesis Inhibitors
  • Oligopeptides
  • probestin
  • CD13 Antigens