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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Small Molecule Antagonists of Integrin Receptors

Author(s): A. Perdih and M. Sollner Dolenc

Volume 17, Issue 22, 2010

Page: [2371 - 2392] Pages: 22

DOI: 10.2174/092986710791698558

Price: $65


The complex and widespread family of integrin receptors is involved in numerous physiological processes, such as tissue remodeling, angiogenesis, development of the immune response and homeostasis. In addition, their key role has been elucidated in important pathological disorders such as cancer, cardiovascular diseases, osteoporosis, autoimmune and inflammatory diseases and in the pathogenesis of infectious diseases, making them highly important targets for modern drug design campaigns. In this review we seek to present a concise overview of the small molecule antagonists of this diverse and highly complex receptor family. Integrin antagonists are classified according to the targeted integrin receptor and are discussed in four sections. First we present the fibrinogen αIIbβ3 and the vitronectin αVβ3 receptor antagonists. The remaining selective integrin antagonists are examined in the third section. The final section is dedicated to molecules with dual or multiple integrin activity. In addition, the use of antibodies and peptidomimetic approaches to modulate the integrin receptors are discussed, as well providing the reader with an overall appreciation of the field.

Keywords: Integrin receptors, fibrinogen (αIIbβ3) receptor, vitronectin (αVβ3) receptor, fibronectin (α5β1) receptor, small molecule antagonists, dual/multiple antagonists

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