Abstract:
Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and
channels involved in pain modulation are able to form receptor heteromers. Receptor and
channel heteromers often display distinct signaling characteristics, pharmacological properties
and physiological function in comparison to monomer/homomer receptor or ion channel
counterparts. It may be possible to capitalize on such unique properties to augment
therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting
heteromers may have greater tissue specificity and analgesic efficacy. This review will
focus on current progress in our understanding of roles of heteromeric GPCRs and channels
in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric
receptors and channels. This approach may be instrumental in the discovery of novel
classes of drugs and expand our repertoire of targets for pain pharmacotherapy.
