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Multiple GPCR and inflammatory targets

Molecular classification
G protein-coupled receptor, Enzyme, Cytokine, Receptor
01

Overview

The term Multiple GPCR and inflammatory targets refers to a broad therapeutic category rather than a single molecular entity. It encompasses a diverse array of G protein-coupled receptors (GPCRs)—the largest family of cell-surface receptors—and various mediators of the inflammatory response, such as cytokines and enzymes like TBK1 and IKKε (Nature Reviews Drug Discovery, 2025). GPCRs are critical for translating extracellular signals into intracellular actions, regulating processes like immune cell recruitment and vascular permeability (Drug Target Review, 2025). Inflammatory targets within this group are central to the pathogenesis of chronic conditions, including asthma, rheumatoid arthritis, and metabolic disorders (NIH, 2024). Drugs associated with this designation, such as Amlexanox, often exhibit polypharmacology by interacting with multiple distinct proteins to achieve a comprehensive anti-inflammatory effect (PubMed, 2023). This multi-target approach is designed to modulate complex signaling networks that single-target agents may fail to control effectively. Because this is a collective term used in drug discovery datasets, it does not correspond to a specific UniProt entry or a single protein structure.

Other names
GPCR and inflammatory mediatorsMulti-target anti-inflammatory profilePolypharmacological inflammatory targets
02

Mechanism of action

Simultaneous modulation of multiple G protein-coupled receptors and inflammatory signaling pathways to achieve synergistic therapeutic effects.

03

Biological functions

Signal transductionImmune responseInflammationResolution of inflammation
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Disease associations

InflammationAutoimmune diseaseCancerMetabolic disease
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Safety considerations

Off-target effectsSystemic immunosuppressionComplex pharmacodynamicsPolypharmacology-related toxicity
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Interacting drugs

Amlexanox

3 more in the full profile.

07

Biomarkers

C-reactive protein (CRP)Interleukin-6 (IL-6)Tumor necrosis factor-alpha (TNF-alpha)

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