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

被引：37

作者：

Pramanik, Dipankar ^{[1
]}

Majeti, Bharat K. ^{[1
]}

Mondal, Goutam ^{[1
]}

Karmali, Priya P. ^{[1
]}

Sistla, Ramakrishna ^{[2
]}

Ramprasad, Obula G. ^{[3
]}

Srinivas, Gunda ^{[3
]}

Pande, Gopal ^{[3
]}

Chaudhuri, Arabinda ^{[1
]}

机构：

[1] Indian Inst Chem Technol, Div Lipid Sci & Technol, Hyderabad 500607, Andhra Pradesh, India

[2] Indian Inst Chem Technol, Div Pharmacol, Hyderabad 500607, Andhra Pradesh, India

[3] Ctr Cellular & Mol Biol, Hyderabad 500607, Andhra Pradesh, India

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 22期

关键词：

D O I：

10.1021/jm800915y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Integrins, the major class of alpha beta heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either alpha(5) or beta(1), integrins have convincingly demonstrated alpha(5)beta(1) integrin to be unquestionably proangiogenic among the 24 known integrin receptors. Herein, we report on a novel RGDK-lipopeptide 1 that targets selectively alpha(5)beta(1) integrin and is capable of targeting genes to mouse tumor vasculatures.

引用

页码：7298 / 7302

页数：5

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