Effect of Transient Receptor Potential (TRP) Channels on G Protein- Coupled Receptors (GPCRS).

Abstract

Pain and nociception are two closely related terms that almost affect us all at one point in our lives. Nociceptors are nerve fibers that conduct pain, on these nociceptors we have different G-protein coupled receptors (GPCRs) such as opioid receptors and transient receptor potential (TRP) channels such as TRPV1 and TRPA1. These receptors and channels are co-expressed in some areas of the body and this project studies the effect of these two TRP channels on the function of opioid receptors. In this project, a BRET (bioluminescence resonance energy transfer) assay was used to detect the protein-protein interaction between the four opioid receptor subtypes and -arrestin2 (Arr3). The findings of this study is that when TRP channels are activated they inhibit the recruitment of Arr3 to the opioid receptor. This will lead to desensitization occurring at a lesser rate and thus may prevent tolerance and addiction to opioids. Understanding the detailed mechanism of how this happens might lead to many advancements in pain management and to understand how GPCRs are affected by TRP channels in more detail.