Lipopeptide with a RGDK Tetrapeptide Sequence Can Selectively Target Genes to Proangiogenic α5β1 Integrin Receptor and Mouse Tumor Vasculature

Integrins, the major class of αβ heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either α5 or β1 integrins have convincingly demonstrated α5β1 integrin to...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2008-11, Vol.51 (22), p.7298-7302
Main Authors: Pramanik, Dipankar, Majeti, Bharat K, Mondal, Goutam, Karmali, Priya P, Sistla, Ramakrishna, Ramprasad, Obula G, Srinivas, Gunda, Pande, Gopal, Chaudhuri, Arabinda
Format: Article
Language:English
Subjects:
Biological and medical sciences
Biotechnology
Fundamental and applied biological sciences. Psychology
Gene therapy
Health. Pharmaceutical industry
Industrial applications and implications. Economical aspects
Medical sciences
Other treatments
Treatment. General aspects
Tumors
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Summary:Integrins, the major class of αβ heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either α5 or β1 integrins have convincingly demonstrated α5β1 integrin to be unquestionably proangiogenic among the 24 known integrin receptors. Herein, we report on a novel RGDK-lipopeptide 1 that targets selectively α5β1 integrin and is capable of targeting genes to mouse tumor vasculatures.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm800915y