Drug intelligence / Profile preview

cRGDyV

Development stage
Preclinical
Modality
Small Molecules, Cyclic Peptides → Modified Peptides → Peptides
Administration
Intravenous
01

Overview

cRGDyV is a synthetic cyclic pentapeptide with the sequence cyclo(Arg-Gly-Asp-D-Tyr-Val). It is a chemically modified version of the RGD (arginine-glycine-aspartic acid) motif, which is recognized by integrin receptors on cell surfaces. The cyclization and inclusion of D-tyrosine enhance its stability, binding affinity, and selectivity for certain integrins—particularly αvβ3 and αvβ5—compared to linear RGD peptides[1][2][5]. By targeting these integrins, which are overexpressed in tumor vasculature and some cancer cells, cRGDyV can inhibit cell adhesion and migration. This makes it valuable as a research tool in studying cell-extracellular matrix interactions, as well as a targeting ligand for drug delivery systems or imaging agents in oncology[1][2][9]. Its mechanism involves competitive inhibition of integrin-ligand interactions.

Other names
cyclic RGDyVcyclo(Arg-Gly-Asp-D-Tyr-Val)c(RGDyV)
02

Targets

αVβ6 (Integrin αVβ6)αVβ3 (Integrin αVβ3)αVβ5 (Integrin αVβ5)GPIIb/IIIa (Integrin alpha-IIb/beta-3)

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