Abstract
Integrin receptors have remained as a key subject of interest in the pharmaceutical industry for the last few years. There are a total of 24 different types of integrin heterodimers. Each of these heterodimers plays important role in various biological processes that are inherent to different pathological conditions. As a result, integrin receptors have been extensively evaluated for their role in therapeutic targeting. There are different classes of inhibitors against integrin receptors and this review provides an overview on different classes of integrin inhibitors that are currently available. A number of review articles have been written on the possible application of integrin receptors in therapeutic targeting. Many of these articles have heavily emphasized on the importance of αvβ3 & αvβ5 receptors as major pharmaceutical target in cancer but little emphasis has been given on the importance of other integrin receptors, such as α5β1, αIIbβ3, α4β7, αvβ6 etc. While this review gives due importance to both αvβ3 & αvβ5 receptors and provides an historical perspective on how these two receptors have evolved as a potential target for cancer, significant emphasis has also been given on the other integrin receptors that have started enjoying the status of important drug target over the course of last few years. Effort has been maintained to discuss briefly on the key physiological basis of their importance as drug target. For example, involvement of αvβ3 in angiogenesis has made it a therapeutic target for the treatment of cancer. At the same time expression of this receptor on the surface of osteoclast has made it a target for the treatment of osteoporosis. Thus, emphasis has been given on discussing the role of the integrin receptors in different disease conditions followed by specific examples of drug molecules that have been trialed against these receptors. While hundreds of candidate molecules have been developed against different integrin receptors only a handful of them has been subject to phase-III clinical trial. That necessitates careful consideration of certain concerns that are associated with direct targeting of integrins and thus has also been an important goal of this review. In the last few years application of integrin receptors have extended beyond mere therapeutic targeting. Several integrin receptors are currently are studied for their potential of aiding at diagnostic imaging and drug delivery. In this review a brief overview has also been provided on how integrin are being targeted for diagnostic imaging and drug delivery with relevant examples. Thus the primary aim of this review has been to provide an comprehensive overview on the broad scope of application that integrin receptors have in the field of medical science.
Highlights
Integrins are cell surface receptors that are primarily involved in integrating the extracellular environment to the intracellular environment as the name suggest [1,2,3]
A special emphasis has been given on αvβ3 & αvβ5, because they remain as the two most extensively explored integrins to date
A number of inhibitors of αvβ3 & αvβ5 have been subject to clinical trials for the treatment of cancer and there are huge numbers of drugs that are being studied at preclinical stage
Summary
Integrins are cell surface receptors that are primarily involved in integrating the extracellular environment to the intracellular environment as the name suggest [1,2,3]. In the last two decades integrins have generated tremendous interest among the scientists. A myriad of articles are being published every year, yet the intricate complexity and diversity of integrin function is continuing to challenge the scientific world. There are a total of 24 different types of integrins [4]. The integrin family of receptors, depending on their ligand recognition pattern can be broadly classified into four different categories—I) RGD binding, II) collagen binding, III) laminin binding, and IV) leukocyte binding types of integrins (Figure 1, adapted from Barczyk et al, 2010). Significant advancements have been made in our understanding of integrin structure
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