Selectin inhibitors

Abstract

The selectins play a significant role in mediating cellular adhesion and thus initiating the inflammatory and cell-mediated immune responses. In an inflammatory response, the selectins mediate the rolling of leukocytes on activated endothelial cells through the recognition of carbohydrate epitopes (e.g., sialyl Lewis^x, sLe^x). The immune response relies on constant recirculation of lymphocytes from the blood through the vascular wall into the tissues and eventually back into the blood. Carbohydrate ligands on high endothelial venules capture circulating lymphocytes via L-selectin-dependent adhesion, leading to transmigration. Although leukocyte recruitment into the tissue is an essential physiological process, uncontrolled recruitment can lead to acute or chronic disorders such as inflammation, autoimmune diseases and tissue rejection during transplantation. Therefore, the development of agents that can modulate selectin-mediated events is an attractive therapeutic area. Summarised in this article are the patents published in this area from 1999 to present.

• inflammation
• inhibitors
• selectins
• sialyl Lewis x
• therapeutics