Uses
RGD-4C is a arginine-glycine-aspartic acid peptide (ACDCRGDCFC) with integrin binding activity. The Arg-Gly-Asp (RGD) sequence serves as the primary integrin recognition site in extracellular matrix proteins, and peptides containing this sequence can mimic the recognition specificity of the matrix proteins. RGD-4C is a αv-integrin ligand, can conjugate with bioactive molecule to exert antitumor effects in animal models[1][2][3].
in vivo
RGD-4C (9.11 mg/kg; injection; single dose) inhibits the growth of B16F10 mouse melanoma in vivo[2].
Modified RGD-4C fused with the N-terminus of plant-derived single-chain ribosome inactivating protein saporin (SAP) (called RGD-SAP), (diluted in sodium chloride, 0.9%; i.v.; 200 μL; every 5 days, for 3 times) exerts anti-tumor activity in a model of muscle invasive bladder cancer[3].
RGD-SAP in combination with mitomycin C, a chemotherapeutic drug, increases the survival of mice bearing orthotopic bladder cancer with no evidence of systemic toxicity[3].
References
[1] Assa-Munt N, et al. Solution structures and integrin binding activities of an RGD peptide with two isomers. Biochemistry. 2001 Feb 27;40(8):2373-8. DOI:
10.1021/bi002101f[2] Yin R, et al. Effect of RGD-4C position is more important than disulfide bonds on antiangiogenic activity of RGD-4C modified endostatin derived synthetic polypeptide. Bioconjug Chem. 2010 Jul 21;21(7):1142-7. DOI:
10.1021/bc900292y[3] Zuppone S, et al. A Novel RGD-4C-Saporin Conjugate Inhibits Tumor Growth in Mouse Models of Bladder Cancer. Front Oncol. 2022 Apr 11;12:846958. DOI:
10.3389/fonc.2022.846958
