Dual regulation by G proteins of agonist‐dependent phosphorylation of muscarinic acetylcholine receptors
[摘要] Muscarinic acetylcholine receptors purified from porcine atrium were phosphorylated, depending on the presence of agonists, by a protein kinase partially purified from porcine brain, which had similar properties to the β-adrenergic receptor kinase. GTP-binding regulatory proteins (Go) had dual effects on the phosphorylation of muscarinic receptors, i.e. stimulation at lower concentrations and inhibition at higher concentrations. The stimulatory effect was reproduced with the βγ subunit of Go and the inhibitory effect with the combination of the α and βγ subunits.
[发布日期] [发布机构]
[效力级别] [学科分类] 生物化学/生物物理
[关键词] Muscarinic receptor;Acetylcholine receptor;GTP-binding regulatory protein;Receptor phosphorylation;β-Adrenergic receptor kinase;Rhodopsin kinase;G protein;GTP-binding regulatory protein;Go;a G protein with α subunit of apparent molecular mass of 39 kDa;[3H]QNB;[3H]L-quinuclidinyl benzylate;GTPγS;guanosine 5 ' -(3-O-thio)triphosphate;SDS-PAGE;sodium dodecyl sulfate polyacrylamide gel electrophoresis;Hepes;4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid;DTT;dithiothreitol [时效性]