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- W2000521278 abstract "G protein βγ subunits have potential as a target for therapeutic treatment of a number of diseases. We performed virtual docking of a small-molecule library to a site on Gβγ subunits that mediates protein interactions. We hypothesized that differential targeting of this surface could allow for selective modulation of Gβγ subunit functions. Several compounds bound to Gβγ subunits with affinities from 0.1 to 60 μM and selectively modulated functional Gβγ-protein-protein interactions in vitro, chemotactic peptide signaling pathways in HL-60 leukocytes, and opioid receptor–dependent analgesia in vivo. These data demonstrate an approach for modulation of G protein–coupled receptor signaling that may represent an important therapeutic strategy." @default.
- W2000521278 created "2016-06-24" @default.
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- W2000521278 date "2006-04-21" @default.
- W2000521278 modified "2023-10-18" @default.
- W2000521278 title "Differential Targeting of Gßγ-Subunit Signaling with Small Molecules" @default.
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- W2000521278 doi "https://doi.org/10.1126/science.1120378" @default.
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