cyclo-rgdyk

Description: Cyclo(RGDyK) trifluoroacetate (TFA), a glycosylated RGD-containing peptide (RGD-peptide), is a potent and selective alphaVbeta3 integrin inhibitor with IC50 of 20 nM. Cyclo(RGDyK) showed high affinity and selectivity for alpha(v)beta3 in vitro (50% inhibitory concentration = 40 nmol/L). Cyclo(RGDyK) conjugation facilitated intracellular drug delivery of polymeric micelles to neovasculature (HUVECs) and tumor cells in which integrin is overexpressed. Cyclo(RGDyK) showed high affinity and selectivity for alphaVbeta3 integrin over alphaVbeta5 and alphaIIbbeta3. In vivo, Cyclo(RGDyK) (1 nM, i.v. injection) blocked the increase of alphaVbeta3 integrin expression in the intima of the left stenotic carotid artery of apoE-/- mice. The favorable biokinetics make the glycosylated RGD-peptide a promising lead structure for tracers to quantify the alpha(v)beta3 expression using PET.

References: J Nucl Med. 2001 Feb; 42(2):326-36; J Drug Target. 2011 Jan; 19(1):25-36.