Where have all the active receptor states gone?
Defining G protein-coupled receptor ligand efficacy and biased agonism in precise chemical terms is one challenge posed by the current structural data that exists for this receptor family. Concepts classically used for understanding enzymes and other nonreceptor proteins may lead us in the right direction.
Department of Pharmacology, Faculty of Medicine, University of Ankara, Ankara, Turkey. ongun.onaran@medicine.ankara.edu.tr
H Ongun
HO
Onaran
Tommaso
T
Costa
D000494:Allosteric Regulation; D000818:Animals; D019393:Arrestin / Q000378:metabolism; D002462:Cell Membrane / Q000737:chemistry / Q000502:physiology; D055808:Drug Discovery; D005786:Gene Expression Regulation / Q000502:physiology; D008024:Ligands; D008958:Models, Molecular; D011485:Protein Binding; D011487:Protein Conformation; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000502:physiology*; D015398:Signal Transduction
D019393:Arrestin; D008024:Ligands; D043562:Receptors, G-Protein-Coupled