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Gi protein signaling pathway

Molecular classification: Signal transduction pathway, G protein-coupled receptor signaling pathway

Overview

The Gi protein signaling pathway is a major intracellular signaling mechanism mediated by G protein-coupled receptors (GPCRs) and heterotrimeric G proteins of the Gi family. Activation of GPCRs coupled to Gi leads to the inhibition of adenylyl cyclase, decreasing cAMP levels. The liberated beta-gamma complex can also activate other effectors like GIRK channels.

Mechanism of action

Pertussis toxin ADP-ribosylates and inactivates Gi/o proteins, disrupting their ability to inhibit adenylyl cyclase and modulate downstream signaling.

Biological functions

Signal transductionRegulation of heart rateRegulation of neuronal excitabilityRegulation of hormone secretion

Disease associations

Whooping cough pathogenesis (indirectly, via Pertussis toxin)

Safety considerations

Disruption of Gi signaling can have broad physiological effects, given its involvement in various regulatory processes.

Interacting drugs

Pertussis toxin

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