Endothelin Receptors

Abstract

Receptors are cellular macromolecules that combine with hormones, neurotransmitters, drugs, or intracellular messengers to initiate a change in cell function, and are thereby concerned directly and specifically in chemical signalling between and within cells. In this article we review the progress that has been made over the past decade in our understanding of various aspects of endothelin receptor (ET receptor) biology. These G protein-coupled receptors are stimulated by the endothelin superfamily of peptides, as well as the sarafotoxins, which are constituents of a rare snake venom (see Chap. 2). There has emerged an enormous body of literature describing the locations of ET receptors within various cell, tissue, and organ systems as well as the myriad of effects produced following their activation. In large part, the great interest in ET receptor biology is generated in response to the likelihood that their activation is linked to the initiation, progression, and symptomology of various disease processes. These aspects of ET receptor biology have been excellently covered in earlier works (Huggins et al. 1993; Rubanyi and Polokoff 1994; Gray and Webb 1996), and detailed, up-to-date accounts of recent findings are described in Chaps. 11–19 in this volume. The focus of this chapter will be to describe some of the important developments that have been made in the fields of ET receptor classification, structure, and ligand binding. Furthermore, it will highlight the important role ET receptors play in fetal development and the extent to which ET receptor expression and function can be modulated by various cytokines, drugs, and in disease.