Inhibition of Transient Receptor Potential Melastatin 3 ion channels by G-protein βγ subunits.

ABSTRACT: Transient receptor potential melastatin 3 (TRPM3) channels are activated by heat, and chemical ligands such as pregnenolone sulphate (PregS) and CIM0216. Here, we show that activation of receptors coupled to heterotrimeric Gi/o proteins inhibits TRPM3 channels. This inhibition was alleviated by co-expression of proteins that bind the βγ subunits of heterotrimeric G-proteins (Gβγ). Co-expression of Gβγ, but not constitutively active Gαi or Gαo, inhibited TRPM3 currents. TRPM3 co-immunoprecipitated with Gβ, and purified Gβγ proteins applied to excised inside-out patches inhibited TRPM3 currents, indicating a direct effect. Baclofen and somatostatin, agonists of Gi-coupled receptors, inhibited Ca²⁺ signals induced by PregS and CIM0216 in mouse dorsal root ganglion (DRG) neurons. Th

SUBMITTER: Badheka D 

PROVIDER: S-EPMC5593506 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature