Date published: 2025-12-24

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Gα o Inhibitors

Gαo inhibitors constitute a distinct chemical class designed to selectively target and modulate the activity of the Gαo protein. Gαo, a member of the G protein family, plays a pivotal role in transducing signals from various cell surface receptors to intracellular effectors. These inhibitors employ diverse chemical structures and mechanisms to impede the function of Gαo within cellular contexts. Researchers have developed compounds that specifically interfere with the activation or signaling cascade involving Gαo, aiming to understand the intricate pathways and cellular processes regulated by this protein.

Compounds identified as Gαo inhibitors typically act by binding to specific sites on Gαo or interfering with the interactions essential for its activation and downstream signaling. These inhibitors exhibit a range of chemical structures, including small molecules or peptide-based compounds, each with its unique mode of action. By disrupting the function of Gαo, these compounds contribute significantly to elucidating the roles played by Gαo in cellular signaling and pave the way for understanding its involvement in various physiological processes.

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A bacterial toxin produced by Bordetella pertussis, it modifies and inhibits Gαi/o proteins by ADP-ribosylation, preventing their interaction with G protein-coupled receptors (GPCRs).

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This compound inhibits Gαi-mediated signaling by blocking the interaction between Gαi and adenylyl cyclase, leading to decreased cAMP production. It has potential in modulating neurotransmission and other GPCR-dependent processes.

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Derived from Chromobacterium sp., this compound selectively inhibits Gαq-mediated signaling by interfering with Gαq binding to phospholipase Cβ. It does not affect Gαi/o signaling.

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A small molecule compound that selectively inhibits Gαi/o-coupled GPCRs by disrupting the interaction between Gαi/o and its downstream effectors. It modulates various GPCR-dependent processes.