CCR2 Receptor Ligands Inhibit Ca v 3.2 T-Type Calcium Channels
Molecular Pharmacology, ISSN: 0026-895X, Vol: 77, Issue: 2, Page: 211-217
2010
- 20Citations
- 27Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations20
- Citation Indexes20
- CrossRef20
- 20
- Captures27
- Readers27
- 27
Article Description
Monocyte chemoattractant protein-1 (MCP-1) is a cytokine known to be involved in the recruitment of monocytes to sites of injury. MCP-1 activates the chemokine (C-C motif) receptor 2 (CCR2), a seven-transmembrane helix G protein-coupled receptor that has been implicated in inflammatory pain responses. Here we show that MCP-1 mediates activation of the CCR2 receptor and inhibits coexpressed N-type calcium channels in tsA-201 cells via a voltage-dependent pathway. Moreover, MCP-1 inhibits Ca v 3.2 calcium channels, but not other members of the Cav3 calcium channel family, with nanomolar affinity. Unlike in N-type channels, this modulation does not require CCR2 receptor activation and seems to involve a direct action of the ligand on the channel. Whole-cell T-type calcium currents in acutely dissociated dorsal root ganglia neurons are effectively inhibited by MCP-1, consistent with the notion that these cells express Ca v 3.2. The effects of MCP-1 were eliminated by heat denaturation. Furthermore, they were sensitive to the application of the divalent metal ion chelator diethylenetriaminepentaacetic acid, suggesting the possibility that metal ions may act as a cofactor. Finally, small organic CCR2 receptor antagonists inhibit Ca v 3.2 and other members of the T-type channel family with micromolar affinity. Our findings provide novel avenues for the design of small organic inhibitors of T-type calcium channels for the treatment of pain and other T-type channel linked disorders.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0026895X24026026; http://dx.doi.org/10.1124/mol.109.059022; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=74549143847&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/19864434; https://linkinghub.elsevier.com/retrieve/pii/S0026895X24026026; https://dx.doi.org/10.1124/mol.109.059022; https://molpharm.aspetjournals.org/content/77/2/211
Elsevier BV
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