The family of G protein-coupled receptors: an example of membrane proteins.
The G protein coupled receptors belong to the largest group of membrane proteins that regulates many essential physiological properties and represents an important class of drug targets. In this chapter, we show how the synergy between a laboratory experiment and computational modeling leads to structural delineation of the ligand binding pocket and how the knowledge of ligand-protein interactions is used for rational local and global drug design in which the structural knowledge of a particular receptor and its ligands is used for drug design of this particular GPCR and others.
Tikhonova
Irina G
IG
INSERM, Institut National de la Santé et de la Recherche Médicale, Université de Toulouse 3, Toulouse, France. tikhonovai@niddk.nih.gov
Fourmy
Daniel
D
D001665:Binding Sites; D002766:Cholecystokinin / Q000378:metabolism; D015195:Drug Design; D008565:Membrane Proteins / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*; D008954:Models, Biological; D008958:Models, Molecular; D016297:Mutagenesis, Site-Directed; D011487:Protein Conformation; D011949:Receptors, Cholecystokinin / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*
D008565:Membrane Proteins; D011949:Receptors, Cholecystokinin; D043562:Receptors, G-Protein-Coupled; D002766:Cholecystokinin