Cilengitide trifluoroacetic acid salt has been used as an inhibitor of integrin ?v?5.
Biochem/physiol Actions
It exhibits antitumor activity in glioblastoma multiforme tumors. Integrins are heterodimers of ? and ? chain. They are transmembrane receptors which are responsible for cell-to-cell and cell-extracellular matrix interactions. They control tumor angiogenesis, invasion and migration.
Cilengitide is a vascular targeting agent (VTA) that acts as an integrin antagonist. Cilengitide is a cyclized Arg-Gly-Glu(RGD)-containing pentapeptide that selectively blocks activation of the Avβ3 and Avβ5 integrins.