The DOI matches its Crossref record; 59 of the 59 references it cites were found in a registry or an index.
Protein Kinase C Activation Regulates Human Serotonin Transporters in HEK-293 Cells via Altered Cell Surface Expression
Open accessAbstract
Antidepressant- and cocaine-sensitive serotonin (5-hydroxytryptamine, 5-HT) transporters (SERTs) dictate clearance of extracellular 5-HT after release. To explore protein kinase C-mediated SERT regulation, we generated a stable human SERT (hSERT)-expressing cell line (293-hSERT) and evaluated modulation of 5-HT activity via studies of 5-HT flux, hSERT-mediated currents under voltage clamp, and surface distribution of SERT protein. 293-hSERT cells exhibit saturable, high-affinity, and antidepressant-sensitive 5-HT uptake as well as hSERT-dependent whole-cell currents. In these cells, the protein kinase C activator β-PMA caused a time-dependent reduction in 5-HT uptake capacity (Vmax) after acute application and a reduction in SERT-mediated currents. Effects of β-PMA were mimicked by the phorbol ester β-PDBu, were not observed with the inactive α-isomers, and could be blocked by treatment of cells with the protein kinase C inhibitor staurosporine. Biotinylation/immunoblot analyses showed that activity reductions are paralleled by a staurosporine-sensitive loss of surface SERT protein. These data indicate that altered surface abundance, rather than reduced catalytic transport efficiency, mediates acute PKC-dependent modulation of 5-HT uptake.
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Cites
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Self-citationMu, delta, and kappa opioid receptor mRNA expression in the rat CNS: An in situ hybridization study
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Cited by
Danbolt, N. C. (2001) · Progress in Neurobiology · doi:10.1016/s0301-0082(00)00067-8 · Cited by 4,227
Plasma membrane monoamine transporters: structure, regulation and function
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Neurotransmitter Receptor and Transporter Binding Profile of Antidepressants and Their Metabolites
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Metadata
- Authors
- Qian, Y., Galli, A., Ramamoorthy, S., Risso, S., DeFelice, L. J., & Blakely, R. D.
- Venue
- The Journal of Neuroscience
- Publisher
- Society for Neuroscience
- Published
- 1997-01-01
- Volume
- 17
- Issue
- 1
- Pages
- 45-57
- ISSN
- 0270-6474 (ISSN-L)
- 1529-2401
- OpenAlex
- W1911240071
- Cited by
- 381
- References
- 59
- FWCI
- 10.13
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Qian, Y., Galli, A., Ramamoorthy, S., Risso, S., DeFelice, L. J., & Blakely, R. D. (1997). Protein Kinase C Activation Regulates Human Serotonin Transporters in HEK-293 Cells via Altered Cell Surface Expression. The Journal of Neuroscience. https://doi.org/10.1523/jneurosci.17-01-00045.1997
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