[Adrenergic receptor and alpha 2 agonist--2: Structure-function relationship of adrenoceptors].
Recombinant DNA experiments using chimeric receptors containing portions of alpha 2 and beta 2 adrenoceptors demonstrated structure-function relationships of adrenoceptors. The seventh transmembrane domain determines the subtype ligand binding specificity between alpha 2 and beta 2 adrenoceptors. A further investigation by mutagenesis suggests that a direct interaction between subtype specific ligands and specific amino acids such as Phe (412) and Asn (312) in the seventh transmembrane domain of the alpha 2 and beta 2 adrenoceptors respectively. The third cytoplasmic loop is responsible for determining the specificity of interactions between the receptor and G protein. Recombinant DNA technology also demonstrated that seven transmembrane domains of adrenoceptors have a counterclockwise arrangement when viewed from the outside of the cell.
Mizobe
T
T
Department of Anesthesiology, Kyoto Prefectural University of Medicine.
D058647:Adrenergic alpha-2 Receptor Agonists; D000818:Animals; D001665:Binding Sites; D019204:GTP-Binding Proteins / Q000378:metabolism; D008024:Ligands; D011485:Protein Binding; D018341:Receptors, Adrenergic, alpha-2 / Q000737:chemistry* / Q000502:physiology; D018343:Receptors, Adrenergic, beta-2 / Q000737:chemistry* / Q000502:physiology; D013329:Structure-Activity Relationship
D058647:Adrenergic alpha-2 Receptor Agonists; D008024:Ligands; D018341:Receptors, Adrenergic, alpha-2; D018343:Receptors, Adrenergic, beta-2; D019204:GTP-Binding Proteins