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Research ArticleArticle

Allosteric Modulation of β2-Adrenergic Receptor by Zn2+

Gayathri Swaminath, Jacqueline Steenhuis, Brian Kobilka and Tae Weon Lee
Molecular Pharmacology January 2002, 61 (1) 65-72; DOI: https://doi.org/10.1124/mol.61.1.65
Gayathri Swaminath
Howard Hughes Medical Institute, Stanford University Medical School, Stanford, California
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Jacqueline Steenhuis
Howard Hughes Medical Institute, Stanford University Medical School, Stanford, California
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Brian Kobilka
Howard Hughes Medical Institute, Stanford University Medical School, Stanford, California
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Tae Weon Lee
Howard Hughes Medical Institute, Stanford University Medical School, Stanford, California
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Abstract

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 μM [Proc Natl Acad Sci USA1997;94:13386–13387; Mol Pharmacol1997;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 β2-adrenergic receptor (β2AR). We found that physiological concentrations of Zn2+ increased agonist affinity and enhanced cAMP accumulation stimulated by submaximal concentrations of the βAR agonist isoproterenol. These results provide evidence that Zn2+ released at nerve terminals may modulate signals generated by the β2AR in vivo.

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Molecular Pharmacology: 61 (1)
Molecular Pharmacology
Vol. 61, Issue 1
1 Jan 2002
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Research ArticleArticle

Allosteric Modulation of β2-Adrenergic Receptor by Zn2+

Gayathri Swaminath, Jacqueline Steenhuis, Brian Kobilka and Tae Weon Lee
Molecular Pharmacology January 1, 2002, 61 (1) 65-72; DOI: https://doi.org/10.1124/mol.61.1.65

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Research ArticleArticle

Allosteric Modulation of β2-Adrenergic Receptor by Zn2+

Gayathri Swaminath, Jacqueline Steenhuis, Brian Kobilka and Tae Weon Lee
Molecular Pharmacology January 1, 2002, 61 (1) 65-72; DOI: https://doi.org/10.1124/mol.61.1.65
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