Dear all,
I'm currently working on establishing the mechanism behind a modulatory effect of a drug candidate on opioid analgesia. We believe that it does so by activating GDP/GTP exchange in the Galpha subunit of the Gi/0 protein. This was confirmed in the GTPgammaS assay. Also, this drug dose-dependently inhibited GTPgammaS stimulation my morphine. My thought was that perhaps this drug promotes coupling of the G protein to a receptor other than the opioid receptor making G proteins less available for morphine stimulation. Are there any commercially available screening assays designed to backtrack which receptors recruit the G-proteins activated by my drug? I would very much like to hear your thoughts on this.
Hi Anna,
I think there are no kits to answer your question. If your assumption on coupling the G protein to another GPCR is right, you might try identifying this receptor via cross-linking the G protein to the GPCR and run an MS analysis to find which GPCRs are cross-linked.
Good luck,
Karoly
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