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Molecular Pharmacology Fast Forward
First published on February 28, 2007; DOI: 10.1124/mol.107.035493


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Received for publication February 26, 2007.
Revised February 26, 2007.
Accepted for publication February 27, 2007.

All Aglow About Presynaptic Receptor Regulation of Neurotransmitter Transporters (Relates to article by Bolan, et al., Fast Forward 31 January 2007)

Randy D. Blakely 1* Louis DeFelice 2

1 Vanderbilt University School of Medicine 2 Vanderbilt University Medical Center

* Address correspondence to: E-mail: randy.blakely{at}vanderbilt.edu

Abstract

Mounting evidence supports the idea that neurotransmitter transporters are subject to many forms of posttranslational regulation typically associated with receptors and ion channels, including receptor and kinase-mediated changes in transporter phosphorylation, cell surface trafficking and/or catalytic activation. Although hints of this regulation can be achieved with traditional radiolabeled substrate flux techniques, higher resolution methods are needed that can localize transporter function in situ as well as permit real-time monitoring of transport function without confounds associated with coincident receptor activation. The elegant study by Bolan et al. capitalizes on the fluorescent properties of a recently introduced substrate for the dopamine (DA) transporter (DAT) termed ASP+, to illuminate a pertusis-toxin sensitive, ERK1/2-dependent pathway by which presynaptic DA D2 receptors (D2Rs) regulate DATs.


Key words: Dopamine, Fluorescence techniques, Regulation - transcriptional





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