7-HELIX RECEPTORS - STRUCTURE AND MODELING

In the past decade there has been an explosion of interest in the study of G protein-coupled receptors, which represent, perhaps, the single most widespread signal transduction system in eukaryotic biology. G protein-coupled receptors are seen as potential pharmacological targets, and thus there is great interest in obtaining structural data that can be used to aid the rational design of selective therapeutic agents. This review provides a general description of the approaches taken towards predicting the structures of some of these receptors. The comparison of the various studies shows that there is a substantial degree of variability in the derived three-dimensional models and in the regions identified as potential sites for ligand binding. This high degree of variability highlights the difficulties of using such models for rational drug design.