Heterotrimeric G proteins, activated by G-protein-coupled receptors (GPCRs), are central mediators of cellular signaling. Activation requires GDP release from the Gα subunit, a step attributed largely to the C-terminal α5 helix, the primary GPCR-interacting region. Contributions from other Gα regions have remained uncl...
Hiroki Arai, Tatsuya Ikuta, Ryoji Kise et al.· Nature Chemical Biology· 0 citations
Cryo-EM is used to capture plausible intermediate states of a viral GPCR-human Gq complex, suggesting a stepwise activation mechanism for G protein activation.
K. Jude, Carl-Mikael Suomivuori, Deepa Waghray et al.· Nature Communications· 0 citations
κ-Opioid receptor (KOR) agonists are promising candidates for analgesic development, yet their clinical application is limited by on-target adverse effects such as sedation and dysphoria. Attenuating β-arrestin2 recruitment while retaining G-protein signaling has therefore attracted interest as a strategy for improving...
Ruburika Nagao, Keita Kajino, Ryoji Kise et al.· European journal of medicina...· 0 citations
Impaired insulin secretion represents a key feature of type 2 diabetes (T2D), a major global health burden. Insulin release from pancreatic β cells is regulated by G protein–coupled receptors linked to different functional classes of G proteins. The potential metabolic role of β cell G12/13 (G12 hereafter) signaling re...
Srinivas Pittala, Liu Liu, Dhanush Haspula et al.· Science Advances· 0 citations
Phospholipase C β (PLCβ) enzymes are activated by heterotrimeric G protein subunits, increasing hydrolysis of phosphatidylinositol-4,5-bisphosphate (PI(4,5)P2) at the plasma membrane. All four human PLCβ isoforms (PLCβ1–4) are activated by Gαq, whereas PLCβ1–3 are activated to varying extents by Gβγ. The binding sites...
Isaac J. Fisher, Kanishka Senarath, Kennedy Outlaw et al.· eLife· 0 citations
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