Activation of heterotrimeric G proteins by G-protein-coupled receptors (GPCRs) requires large-scale opening of the Gα α-helical domain (AHD) to expose the nucleotide-binding site and facilitate GDP–GTP exchange. Although orthosteric ligands are known to modulate GPCR conformation, how these effects propagate to the bou...
Jonathan C. Deutsch, Daniel Hilger, John Janetzko et al.· Nature Structural & Molecula...· 1 citation
N-hydroxyapiosporamide (NHAP) is established as a first-in-class Gi-selective inhibitor, providing a cell-permeable chemical scaffold for the optimization of next-generation agents to control Gi-signaling in cell-based systems and, ultimately, to target Gαi1-driven pathologies.
A. Naimi, Tim Berger, Philipp Dahlhaus et al.· bioRxiv· 0 citations
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