ABSTRACT
Drugs that selectively inhibit the formation or action of leukotrienes (LT) are currently being introduced as new therapy in asthma. The primary structure of the enzymes in the 5-lipoxygenase (5-LO) pathway has been defined and great progress has been made with respect to the understanding of their cellular localization and genomic regulation (reviewed in Ref. 1). In the process of developing drugs for inhibition of leukotrienes, FLAP (5-lipoxygenase activation protein) was discovered as an important cofactor and rational target for interference with biosynthesis (2,3). In contrast, despite the development of several potent antagonists of cysteinyl-leukotrienes, the corresponding molecular information about the receptors for leukotrienes is very limited. The available leukotriene receptor antagonists have been developed by conventional screening of new chemical entities in functional or ligand-binding assays. The knowledge about leukotriene receptors is mainly derived from studies of functional responses. This chapter will present the framework that defines our current understanding of leukotriene receptors and raise some of the issues that future research will need to address.
