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

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• 作者：Dipankar Pramanik ; Bharat K. Majeti ; Goutam Mondal ; Priya P. Karmali ; Ramakrishna Sistla ; Obula G. Ramprasad ; Gunda Srinivas ; Gopal Pande ; Arabinda Chaudhuri
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：November 27, 2008
• 年：2008
• 卷：51
• 期：22
• 页码：7298-7302
• 全文大小：225K
• 年卷期：v.51,no.22(November 27, 2008)
• ISSN：1520-4804

文摘

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.