| Identification | Back Directory | [Name]
ACDCRGDCFCG (DISULFIDE BRIDGE: 2-10 AND 4-8) | [CAS]
332179-76-7 | [Synonyms]
RGD-4C
ACDCRGDCFCG (DISULFIDE BRIDGE: 2-10 AND 4-8)
H-Ala-Cys-Asp-Cys-Arg-Gly-Asp-Cys-Phe-Cys-Gly-OH(Cys2-Cys10 , Cys4-Cys8)
H-ALA-CYS-ASP-CYS-ARG-GLY-ASP-CYS-PHE-CYS-GLY-OH (DISULFIDE BRIDGE: 2-10 AND 4-8)
ALA-CYS-ASP-CYS-ARG-GLY-ASP-CYS-PHE-CYS-GLY(DISULFIDE BRIDGE:CYS2-CYS10, CYS4-CYS8) | [Molecular Formula]
C42H64N14O16S4 | [MDL Number]
MFCD04974399 | [MOL File]
332179-76-7.mol | [Molecular Weight]
1149.3 |
| Hazard Information | Back Directory | [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 |
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