Therapeutic ReviewsArginine-Glycine-Aspartate–Binding Integrins as Therapeutic and Diagnostic TargetsSun, Cui-Cui PhD1; Qu, Xian-Jun MD, PhD1,2,*; Gao, Zu-Hua MD, PhD2,3,4Author Information 1Department of Pharmacology, Key Laboratory of Chemical Biology, School of Pharmaceutical Sciences, Shandong University, Jinan, China; 2Department of Pharmacology, School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing, China; 3Department of Pathology, McGill University, Montreal, Canada; and 4Department of Pathology, Beijing YouAn Hospital, Capital Medical University, Beijing, China. Address for correspondence: Department of Pharmacology, Key Laboratory of Chemical Biology, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China. E-mail: [email protected] The authors have no conflicts of interest to declare. Supported by Research Institute of McGill University Health Center. American Journal of Therapeutics: January/February 2016 - Volume 23 - Issue 1 - p e198-e207 doi: 10.1097/MJT.0000000000000053 Buy Metrics Abstract Arginine-glycine-aspartate (RGD)–binding integrins, including αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, α5β1, αIIbβ3, and α8β1, recognize the tripeptide motif RGD in their ligands. RGD-binding integrins are involved in various cell functions, including cell proliferation, survival, differentiation, and motility that are critically important to both health and disease. The diagnostic and therapeutic value of some RGD-binding integrin inhibitors are either clinically proven or at different stages of development. In this review, we first summarized the structure and signaling characteristics of RGD-binding integrins. We then discussed the functions of RGD-binding integrins and their association with human disease. Finally, we recapitulated the research efforts and clinical trials of targeting RGD-binding integrins for the diagnosis and treatment of human disease. This comprehensive review of the current advances in RGD-binding integrins could assist scientists and clinicians in gaining a complete understanding of this group of molecules. It can also contribute to the design of new projects to further advance this field of research and to better apply the research results to benefit patients in clinical practice. Copyright © 2016 Wolters Kluwer Health, Inc. All rights reserved.