Development of tripeptidyl farnesyltransferase inhibitors

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1599-602. doi: 10.1016/s0960-894x(02)00227-5.

Abstract

The first example of tripeptide inhibitors of farnesyltransferase with sub-micromolar inhibition activity was developed based on the fact that CVFM is not a substrate for farnesyltransferase.

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Amino Acid Sequence
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Farnesyltranstransferase
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology*

Substances

  • Enzyme Inhibitors
  • Oligopeptides
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase