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Nip it in the vessel

Researchers have created a novel molecule that helps stop the growth of new blood vessels that nourish vicious tumours1. The novel molecule consisting of a lipid connected to a peptide delivers an anti-cancer gene via a cell surface protein that aids in the growth of new blood vessels. The delivered anti-cancer gene ultimately inhibits tumour growth.

Angiogenesis, the sprouting of new blood vessels from pre-existing vessels, is a remarkable feature of tumor growth. Prevention of new blood vessel formation around tumor tissues is a promising therapeutic approach to combat cancers. Recent studies have identified integrins, a type of cell surface proteins (receptor) and molecular markers as potential drug targets in cancers. Integrins have been shown to play a role in the growth of new blood vessels around tumour.

For the study, the researchers synthesized a lipopeptide known as RGDK-lipopeptide-1. Of the integrins, they chose alpha5beta1 integrin receptor, which has been shown to aid angiogenesis. The research team delivered a complex of an anti-cancer gene (p53) and RGDK-lipopeptide-1 into mice bearing a type of aggressive tumour (B16F1). The study found remarkable inhibition of tumour growth in mice.

The researchers believe that this newly developed RGDK-lipopeptide is a powerful addition to the existing vehicles for delivering anti-cancer genes or drugs in anti-angiogenic cancer therapy selectively via α5β1 integrin receptors.

"This new lipopeptide is also expected to find use in non-invasive imaging of the network of blood vessels around tumour," says lead researcher Arabinda Chaudhuri. Research is under progress towards understanding how the administration of RGDK-lipopeptide anti-cancer gene complex inhibits the tumor growth, he adds.

The authors of this work are from: Division of Lipid Science and Technology, Pharmacology Division, Indian Institute of Chemical Technology, Hyderabad, India, Centre for Cellular and Molecular Biology, Hyderabad, India.



  1. Pramanik, D. et al. Lipopeptide with a RGDK Tetrapeptide Sequence Can Selectively Target Genes to Proangiogenic α5β1 Integrin Receptor and Mouse Tumor Vasculature. J. Med. Chem. (2008) doi: 10.1021/jm800915y

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