Agonizing Integrin Antagonists?

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Agonizing Integrin Antagonists? Sara M. Weis, Dwayne G. Stupack, David A. Cheresh  Cancer Cell  Volume 15, Issue 5, Pages 359-361 (May 2009) DOI: 10.1016/j.ccr.2009.04.005 Copyright © 2009 Elsevier Inc. Terms and Conditions

Figure 1 Balance of Integrin Activation Regulates Cell Movement between Tissue Microenvironments Activity of αv integrins can be modulated by binding to soluble integrin ligand, leading to changes in cell behavior. High doses of RGD-mimetic integrin inhibitors act as integrin antagonists and antiangiogenic agents, whereas low doses of the same drugs paradoxically activate αv integrins to promote migration, invasion, and angiogenesis. The signals produced by endogenous RGD-containing ECM proteins and soluble fragments can thereby be outcompeted by exposure to μM doses of RGD-mimetic drugs. Cancer Cell 2009 15, 359-361DOI: (10.1016/j.ccr.2009.04.005) Copyright © 2009 Elsevier Inc. Terms and Conditions