Allosteric modulation of β2-adrenergic receptor by Zn2+

被引：81

作者：

Swaminath, G ^{[1
]}

Steenhuis, J ^{[1
]}

Kobilka, B ^{[1
]}

Lee, TW ^{[1
]}

机构：

[1] Stanford Univ, Sch Med, Howard Hughes Med Inst, Stanford, CA 94305 USA

来源：

MOLECULAR PHARMACOLOGY | 2002年 / 61卷 / 01期

关键词：

D O I：

10.1124/mol.61.1.65

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Zn2+ is abundant in the brain, where it plays a role in the function of a number of enzymes, structural proteins, and transcription factors. Zn2+ is also found in synaptic vesicles and is released into synapses achieving concentrations in the range of 100 to 300 muM [Proc Nat/Acad Sci USA 1997;94:13386-13387; Mol Pharmacol 1997;51:1015-1023]. Therefore, Zn2+ may play a physiological role in regulating the function of postsynaptic channels and receptors. We characterized the effect of Zn2+ on the functional properties of the beta(2)-adrenergic receptor (beta(2)AR). We found that physiological concentrations of Zn2+ increased agonist affinity and enhanced cAMP accumulation stimulated by submaximal concentrations of the betaAR agonist isoproterenol. These results provide evidence that Zn2+ released at nerve terminals may modulate signals generated by the beta(2)AR in vivo.

引用

页码：65 / 72

页数：8

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