ArticleACS pharmacology & translational science2025
Critical Residues in the Gβ Subunit Mediate Selective Recruitment of the Gαq Heterotrimer to Activated G Protein-Coupled Receptors.
Article in ACS pharmacology & translational science, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
G protein-coupled receptors (GPCRs), the largest family of membrane proteins, serve as primary targets for over 30% of FDA-approved drugs. While signaling bias among Gα subtypes is well characterized, emerging evidence highlights that Gβγ subtypes govern the coupling of the Gα heterotrimer to GPCRs. However, whether Gβγ subtype selectivity depends on the receptor or the Gα subunit and the underlying mechanism remain unresolved. Here, we focused on Gαq-coupled GPCRs and investigated Gβγ preferences using bioluminescence resonance energy transfer assays to assess Gβγ selectivity along with Gαq-GPCR coupling and calcium flux assays to measure downstream Ca
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