Adhesion molecules participate in many stages of immune response; they regulate leukocyte circulation, lymphoid cell homing to tissues and inflammatory sites, migration across endothelial cells and T-cell stimulation. During Tcell immune response, adhesion molecules form a specialized junction between T-cell and the antigen presenting cell. Thus, many researchers have focused their attention on targeting adhesion molecules for developing therapeutic agents. Most of these efforts are intended to develop drugs for autoimmune and inflammatory diseases. Therapeutic agents like efalizumab and alefacept have been approved by the FDA for the treatment of inflammatory autoimmune diseases. This review focuses on some of the basic aspects and importance of adhesion molecules, recent understanding of the structure of adhesion molecules, and the targeted therapeutic agents.