EndothelinA-endothelinB receptor cross-talk and endothelin receptor binding

Abstract

The magnitude of inhibition of an endothelin (ET)-1 response by selective blockade of the ET(A) or ET(B) receptors can be limited by apparent compensation mediated by the unblocked receptor. While the mechanism underlying this functionally defined interaction, or 'cross-talk', is not clear, binding studies suggest an interaction between the ET receptor subtypes. These binding studies are reviewed and suggest that, in general, they support the hypothesis that ET(A) and ET(B) receptor activation of intracellular signalling pathways influence ET-1 binding to these receptor subtypes. However, the relationship of these binding studies to functional effects and, thus, functional ET(A)-ET(B) receptor cross-talk, remains largely untested.