Product Spotlight for 10/8/19: "ONcological TARGETing: Revisiting the RGDs"

The integrins are involved in many cellular processes including cell proliferation and differentiation and act as receptors for cell-adhesion molecules. A particular group of integrins are called the RGD-binding integrins and are named for the Arg-Gly-Asp (RGD) in their sequence.  This sequence is a cell attachment site and is recognized by several integrins. Many strategies for fighting diseases, such as cancer, target these RGD-binding integrins because they are easily accessible and inhibited by peptides, peptidomimetics, and monoclonal antibodies.1

With the advent of “click chemistry”, RGD peptides can have a lysine side chain amine converted to an azide for easy functionalization (see RGD-3759-PI). In cancer tumor imaging, several radiolabeled, cyclic RGD peptides have been found to be useful in integrin αvβ3-targeting. Integrin αvβ3 binding affinity is also increased by using a bicyclic RGD peptide.2-5 Peptides International is a known leader in RGD peptide products, especially dimeric and larger dendrimers of RGD peptides, all of which are part of its RGD Technology Platform. Peptides International now offers a RGD-PEG-PEG-azide peptide which is optimized for Click chemistry and facile synthesis of dendrimeric platforms with the corresponding alkyne component using a branching strategy. An example of a branching strategy of this type could use a template such as 5-hexynoyl-Lys(5-hexynoyl)-Gly-Lys(hexynoyl)-Gly-Lys(hexynoyl)-NH2. This would allow for preparation of the tetrameric form of the RGD dendrimer.

We urge you to explore all the RGD products and services we offer including our comprehensive RGD Technology Platform, a holistic approach that designed to support you from conception to market reality.

A selection of our RGD products:

NEW! RGD Peptides:


Control Peptide for RGD-3000-PI

Clickable RGD Peptides:

Clickable RGD for Dendrimer Constructs

Bicyclic RGD Peptide Optimized for Click Chemistry  

Dimeric RGD Peptide for Click Chemistry

Linear RGD Peptides:

Fibronectin Active Fragment (RGDS)
PFA-4171, PFA-4171-v (0.5 mg vial)
Arg-Gly-Asp-Ser ● ½AcOH ● 2H2O


Cell-Penetrating RGD peptide:

Ac-cyclo [Pen-Tyr(Me)-Ala-Arg-Gly-Asp-Asn-Tic-Cys]-NH₂
Cell-Penetrating Peptide that Targets EGFR, Binds to a Specific Protein in Carcinoma Cells, and Induces Apoptosis

Cyclic RGD peptides:

αvβ3 Integrin Binding RGD Peptide RGD Tumor Targeting Peptide

RGD Tumor Targeting Peptide (linker additions via Cys)

Cilengitide: Cyclo(Arg-Gly-Asp-D-Phe-N-Me-Val)
Selective Inhibitor of αvβ3 and αvβ5 with Possible Role in Tumor Therapy

View our complete list of RGD products
Read more about our RGD peptides
Read about Two Bicyclic RGD Peptides Optimized for Click Chemistry
Learn more about Click Chemistry


  1. C.-C. Sun, X.-J. Qu, & Z.-H. Gao, American Journal of Therapeutics, 23, e198 (2016).
  2. M. Colombo and A. Bianchi, Molecules, 15(1), 178 (2010).
  3. J. Shi, F. Wang, S. Liu, Biophysics Reports, 2(1), 1 (2016).
  4. S. Liu, Bioconjug Chem., 26(8),1413 (2015).
  5. S. Liu, Bioconjug Chem., 20(12), 2199 (2010).