Target intelligence / Profile preview

Free fatty acid receptor 2 (FFAR2), Free fatty acid receptor 3 (FFAR3), Hydroxycarboxylic acid receptor 2 (HCA2) (FFAR2, FFAR3, HCA2)

Target
FFAR2, FFAR3, HCA2
Molecular classification
G protein-coupled receptor, Cell surface receptor, Nutrient sensor
01

Overview

The butyric acid GPCRs are a group of G protein-coupled receptors activated by butyric acid, primarily including Free Fatty Acid Receptor 2 (FFAR2), Free Fatty Acid Receptor 3 (FFAR3), and Hydroxycarboxylic Acid Receptor 2 (HCA2). These receptors are key mediators of the effects of short-chain fatty acids produced by gut microbiota and play pivotal roles in immune regulation, inflammation, energy balance, and metabolic homeostasis. Activation of these receptors by butyrate leads to anti-inflammatory effects, modulation of intestinal barrier function, and beneficial metabolic consequences. Due to these roles, FFAR2, FFAR3, and HCA2 are of strong therapeutic interest in inflammatory diseases, metabolic syndrome, cancer, and cardiovascular conditions, although no approved drugs targeting them currently exist[1][2][6].

Other names
FFAR2 (GPR43)FFAR3 (GPR41)HCA2 (GPR109A, Hydroxycarboxylic acid receptor 2)
02

Mechanism of action

Agonists like butyric acid activate these receptors, mediating anti-inflammatory, metabolic, and immune-modulatory effects primarily via Gi/o protein-coupled pathways[2][6].

03

Biological functions

Signal transductionImmune responseRegulation of inflammationMaintenance of intestinal barrier functionRegulation of energy metabolism
04

Disease associations

InflammationCancerCardiovascular diseaseMetabolic disorders (e.g., diabetes, obesity)
05

Safety considerations

No major safety concerns identified for receptor modulation in clinical research; challenges include specificity, off-target effects, and optimal dosing[6].
06

Interacting drugs

Butyric acid (endogenous agonist)

2 more in the full profile.

07

Biomarkers

Butyrate/short-chain fatty acid levels (indirect)Expression levels of FFAR2, FFAR3, HCA2 in relevant tissues (for research use)

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