Fishman P H, Perkins J P
Membrane Biochemistry Section, National Institute of Neurological and Communicative Disorders and Stroke, Bethesda, Maryland 20892.
Adv Second Messenger Phosphoprotein Res. 1988;21:25-32.
Although desensitization of the beta AR-coupled adenylate cyclase system has been stressed in this chapter, it appears to be a useful model. Carbachol induces sequestration of muscarinic receptors in several cell lines. More recently, agonist-mediated phosphorylation of muscarinic receptors in chick heart has been observed. Based on the predicted amino acid sequence from the recently cloned cDNA, the muscarinic receptor resembles beta AR and rhodopsin with seven membrane-spanning regions and several potential phosphorylation sites in the carboxy-terminal region. Thus, receptor phosphorylation and sequestration may be a general mechanism of desensitization.
尽管本章着重讨论了β肾上腺素能受体偶联腺苷酸环化酶系统的脱敏作用,但它似乎是一个有用的模型。卡巴胆碱可诱导几种细胞系中毒蕈碱受体的隔离。最近,在鸡心脏中观察到激动剂介导的毒蕈碱受体磷酸化。根据最近克隆的cDNA预测的氨基酸序列,毒蕈碱受体类似于β肾上腺素能受体和视紫红质,具有七个跨膜区域,并且在羧基末端区域有几个潜在的磷酸化位点。因此,受体磷酸化和隔离可能是脱敏的一般机制。