ABSTRACT

Disintegrins comprise a family of low-molecular-weight non-enzymatic integrin antagonists that are broadly distributed in viperid (vipers and rattlesnakes) venoms. In the last decade, disintegrin research has progressed tremendously and is proving to be critical for understanding the biology and evolution of viperid venoms. In addition, the structural and functional diversity of disintegrins makes them ideal molecules for elucidating novel information on structural determinants involved in integrin recognition and function, which has relevance for both basic and clinical research. In this chapter, we review the current understanding of the evolutionary history and the structural/functional relationships of disintegrins. We also address a unique and surprising biological role of disintegrins and highlight some of the most promising and more recent studies that have explored the therapeutic potential of these compounds.