Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds

Org Biomol Chem. 2005 Dec 21;3(24):4392-4. doi: 10.1039/b513145f. Epub 2005 Nov 15.


Structure-activity relationship studies on CXCR4 antagonists, which were previously found by using cyclic pentapeptide libraries, were performed to optimize side-chain functional groups, involving conformationally constrained analogues. In addition, a new lead of cyclic pentapeptides with the introduction of a novel pharmacophore was developed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Inhibitory Concentration 50
  • Molecular Structure
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / pharmacology*
  • Receptors, CXCR4 / antagonists & inhibitors*
  • Receptors, CXCR4 / metabolism*
  • Structure-Activity Relationship


  • Peptides, Cyclic
  • Receptors, CXCR4
  • cyclo(tyrosyl-arginyl-arginyl-3-(2-naphthyl)alanyl-glycyl)