Product of the Month: cyclo-Arg-Gly-Asp (RGD) Peptides

Product of the Month: cyclo-Arg-Gly-Asp (RGD) Peptides

Published on 22/06/2020

The integrin receptor interacting RGD sequence and related peptides act as promising tools for drug therapy and cancer research. Find more information on our portfolio of cyclic RGD peptides.

Integrins are a family of structurally, immunochemically, and functionally related heterodimeric cell-surface receptors mediating adhesion between cells and the extracellular matrix (ECM) by binding to ligands with an exposed arginine-glycine-aspartate (RGD) sequence. Integrins also stimulate intracellular signaling and gene expression involved in cell growth, migration, and survival. If not properly process-regulated, integrins are found to be related to diseases such as thrombosis, inflammation, and cancer. Specifically, the RGD motif is recognized by integrins ανβ3 and ανβ5 which are overexpressed in many tumors and thus have become promising diagnostic indicators and therapeutic targets.

Iris Biotech offers a variety of cyclic RGD peptides which are conformationally rigid and typically display enhanced metabolic stability over their linear counterparts.

One example possessing very high affinity for the αvβ3 integrin is the dimeric peptide E[c(RGDfK)]2 (LS-3980), that consists of two cyclic pentapeptides c(RGDfK) linked by a glutamic acid residue. Thus, this dimeric RGD peptide shows high tumor targeting properties. It serves as an integrin inhibitor and gained interest in non-small-cell lung cancer treatment. It can be easily conjugated to drug molecules, chelators, or dyes. In this context, please see LS-3950 (ICG-E[c(RGDfK)]2), the ICG conjugate of LS-3980 combining the fluorescent properties of ICG and the favorable αvβ3-binding capabilities of LS-3980 allowing tumor targeting.

Cyclo-[RGDfK(TPP)] (LS-3920) serves as cyclic RGD peptide for the preparation of multicellular tumor spheroids (MTS) – 3D in vitro models that mimic the in vivo tumor environment.

In case you don’t find your desired derivative in our Webshop, send your inquiry to our Custom Synthesis Service!


  • RGD and Other Recognition Sequences for Integrins; E. Ruoslahti; Annu Rev Cell Dev Biol. 1996; 12: 697-715.
  • Integrins: A Family of Cell Surface Receptors; R. O. Hynes; Cell 1987; 48: 549-54.
  • Cyclic Peptides: Promising Scaffolds for Biopharmaceuticals; D. Gang, D. W. Kim, H.-S. Park; Genes 2018; 9: 557.
  • Tumor targeting with radiolabeled alpha(v)beta(3) integrin binding peptides in a nude mouse model. M. L. Janssen, W. J. Oyen, I. Dijkgraaf, L. F. Massuger, C. Frielink, D. S. Edwards, M. Rajopadhye, H. Boonstra, F. H. Corstens and O. C. Boerman; Cancer Res. 2002; 62(21): 6146-6151.
  • microPET imaging of glioma integrin alpha(v)beta(3) expression using (64)Cu-labeled tetrameric RGD peptide. Y. Wu, X. Zhang, Z. Xiong, Z. Cheng, D. R. Fisher, S. Liu, S. S. Gambhir and X. Chen; J. Nucl. Med. 2005; 46(10): 1707-1718.
  • 3D in vitro co-culture models based on normal cells and tumor spheroids formed by cyclic RGD-peptide induced cell self-assembly; R. Akasov, A. Gileva, D. Zaytseva-Zotova, S. Burov, I. Chevalot, E. Guedon and E. Markvicheva; Biotechnol. Lett. 2017; 39: 45-53.
  • Sialylation facilitates self-assembly of 3D multicellular prostaspheres by using cyclo-RGDfK(TPP) peptide; S. Haq, V. Samuel, F. Haxho, R. Akasov, M. Leko, S. V. Burov, E. Markvicheva and M. R. Szewczuk; OncoTargets Ther 2017; 10: 2427-2447.
  • Sialylation transmogrifies human breast and pancreatic cancer cells into 3D multicellular tumor spheroids using cyclic RGD-peptide induced self-assembly; R. Akasov, S. Haq, F. Haxho, V. Samuel, S. V. Burov, E. Markvicheva, R. J. Neufeld and M. R. Szewczuk; Oncotarget 2016; 7: 66119-66134.
  • Formation of multicellular tumor spheroids induced by cyclic RGD-peptides and use for anticancer drug testing in vitro; R. Akasov, D. Zaytseva-Zotova, S. Burov, M. Leko, M. Dontenwill, M. Chiper, T. Vandamme and E. Markvicheva; Int. J. Pharm. 2016; 506: 148-157.
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