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G protein-coupled receptor modulator

Overview

G protein-coupled receptor (GPCR) modulators are molecules (often drugs or endogenous ligands) that alter the activity of GPCRs. GPCRs are a large and diverse family of integral membrane proteins that play a central role in cellular signal transduction. They respond to a wide variety of external signals—including hormones, neurotransmitters, sensory stimuli, and more—by activating intracellular signaling pathways via heterotrimeric G proteins.

Mechanism of action

Modulation of G protein-coupled receptor activity via agonism, antagonism, inverse agonism, or allosteric modulation.

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