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Ligands Exert Biased Activity to Regulate Sigma 1 Receptor Interactions With Cationic TRPA1, TRPV1, and TRPM8 Channels.

Front Pharmacol. 2019; 
Cortés-Montero E, Sánchez-Blázquez P, Onetti Y, Merlos M, Garzón J.
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Gene Synthesis … Having demonstrated that the σ1R and HINT1 do not bind to GST (#Z02039; GenScript Co, USA) (see Supplementary Figure 1) (Sánchez-Blázquez et al, 2012), we assessed the association of GST-free σ1Rs or HINT1 with the GST-tagged TRP cytosolic sequences … Get A Quote

摘要

The sigma 1 receptor (σ1R) and the mu-opioid receptor (MOR) regulate the transient receptor potential (TRP) V1 calcium channel. A series of proteins are involved in the cross-regulation between MORs and calcium channels like the glutamate N-methyl-D-aspartate receptor (NMDAR), including the histidine triad nucleotide-binding protein 1 (HINT1), calmodulin (CaM), and the σ1R. Thus, we assessed whether similar mechanisms also apply to the neural TRP ankyrin member 1 (TRPA1), TRP vanilloid member 1 (TRPV1), and TRP melastatin member 8 (TRPM8). Our results indicate that σ1R and CaM bound directly to cytosolic regions of these TRPs, and this binding increased in the presence of calcium. By contrast, the associatio... More

关键词

N-methyl-D-aspartate receptor; calmodulin; histidine triad nucleotide-binding protein 1; ligand bias; transient receptor potential ankyrin member 1; transient receptor potential melastatin member 8; transient receptor potential vanilloid member 1; type 1 sigma receptor