Allosteric modulators of class-C G-protein-coupled receptors open new possibilities for therapeutic application

Abstract

The two main neurotransmitters, glutamate and GABA, as well as calcium ions, sweet taste molecules and some pheromones, act on class-C G-protein-coupled receptors (GPCRs). These natural ligands bind within the large extracellular domain of these receptors. Recently, both negative and positive allosteric modulators have been identified for many of these receptors. These compounds bind in the heptahelical domain and possess several specific properties that make them good candidates for multiple therapeutic and industrial applications. © 2004 Elsevier Ltd. All rights reserved.