Theranostics 2011; 1:154-188. doi:10.7150/thno/v01p0154 This volume


Integrin Targeted Therapeutics

Melissa Millard, Srinivas Odde, Nouri Neamati

Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, PSC304 1985 Zonal Avenue, Los Angeles, CA 90089

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Millard M, Odde S, Neamati N. Integrin Targeted Therapeutics. Theranostics 2011; 1:154-188. doi:10.7150/thno/v01p0154. Available from

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Integrins are heterodimeric, transmembrane receptors that function as mechanosensors, adhesion molecules and signal transduction platforms in a multitude of biological processes. As such, integrins are central to the etiology and pathology of many disease states. Therefore, pharmacological inhibition of integrins is of great interest for the treatment and prevention of disease. In the last two decades several integrin-targeted drugs have made their way into clinical use, many others are in clinical trials and still more are showing promise as they advance through preclinical development. Herein, this review examines and evaluates the various drugs and compounds targeting integrins and the disease states in which they are implicated.

Keywords: Integrin-targeted therapeutics, abciximab, tirofiban, eptifibatide, natalizumab, cilengitide, abegrin, acute coronary syndromes, Multiple Sclerosis, Crohn's Disease, cancer, angiogenesis, osteoporosis, age related macular degeneration, integrin-targeted small molecules, integrin-targeted peptides, integrin-targeted therapeutic antibodies