NC-100717: a versatile RGD peptide scaffold for angiogenesis imaging

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6190-3. doi: 10.1016/j.bmcl.2006.09.033. Epub 2006 Sep 26.


Targeting the molecular pathways associated with angiogenesis offers great potential in detecting disease pathology using in vivo imaging technologies. Initiation of angiogenesis requires activation and migration of endothelial cells in order for neovascularization to proceed. Endothelial cells associate with the extracellular matrix through specific interactions with a variety of cell adhesion receptors known as integrins. Peptides containing the tripeptide sequence RGD are known to bind with high affinity to the alphavbeta3 and alphavbeta5 integrins associated with angiogenesis. We present herein the synthesis and in vitro binding affinity of the RGD-containing peptide NC-100717 and a range of molecular probes derived from this intermediate.

MeSH terms

  • Angiogenic Proteins / chemistry
  • Angiogenic Proteins / pharmacology*
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology*
  • Extracellular Matrix / drug effects
  • Extracellular Matrix / physiology
  • Humans
  • Integrin alphaVbeta3 / drug effects
  • Integrin alphaVbeta3 / physiology
  • Models, Molecular
  • Neovascularization, Physiologic*
  • Oligopeptides / chemistry*
  • Peptides, Cyclic / pharmacology*


  • Angiogenic Proteins
  • Integrin alphaVbeta3
  • NC 100717
  • Oligopeptides
  • Peptides, Cyclic
  • arginyl-glycyl-aspartic acid