RGD-4C trifluoroacetate salt

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].

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> Integrin

RGD-4C (2.5, 5, 10 μg/mL) inhibits BAE cell proliferation by synthetic form modified with endostatin-derived peptides[2].

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].

[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.  

[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.  

[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.