Target intelligence / Profile preview

Unsaturated fatty acid (UFA)

Target
UFA
Molecular classification
Other, Lipid, Carboxylic acid
01

Overview

Unsaturated fatty acids (UFAs) are long-chain carboxylic acids containing one or more double bonds, categorized primarily into monounsaturated (MUFAs) and polyunsaturated (PUFAs) fatty acids [2, 10]. They are fundamental components of biological systems, serving as essential structural elements of cell membranes and as critical sources of energy [1, 8]. Beyond these roles, UFAs act as potent signaling molecules and endogenous ligands for several therapeutic targets, including the G protein-coupled receptors FFAR1 (GPR40) and FFAR4 (GPR120), as well as nuclear receptors like the peroxisome proliferator-activated receptors (PPARs) [13, 17, 19]. Through these pathways, they modulate inflammatory responses, glucose homeostasis, and lipid metabolism [3, 24]. Clinically, specific UFAs such as eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are used as pharmaceutical agents to treat severe hypertriglyceridemia and reduce cardiovascular risk [14, 23]. However, their use is associated with therapeutic challenges, including potential increases in bleeding time and the risk of atrial fibrillation at high doses [12, 16].

Other names
PUFAMUFAPolyunsaturated fatty acidMonounsaturated fatty acidEssential fatty acidOmega fatty acid
02

Mechanism of action

Activation of free fatty acid receptors (FFAR1, FFAR4) and peroxisome proliferator-activated receptors (PPARs); competitive displacement of arachidonic acid from cell membranes to reduce pro-inflammatory eicosanoid synthesis; and inhibition of hepatic VLDL synthesis and lipogenesis [13, 15, 17, 19].

03

Biological functions

Signal transductionCell membrane integrityEnergy metabolismGene expression regulationImmune response
04

Disease associations

Cardiovascular diseaseInflammationMetabolic syndromeNeurodegenerative diseaseCancer
05

Safety considerations

Increased risk of bleedingRisk of atrial fibrillation or flutterElevation of low-density lipoprotein (LDL) cholesterolGastrointestinal side effects (e.g., dyspepsia, fishy eructation)Fish or shellfish allergy
06

Interacting drugs

Icosapent ethyl

6 more in the full profile.

07

Biomarkers

Serum triglyceride levelOmega-3 indexEicosapentaenoic acid (EPA) plasma concentrationDocosahexaenoic acid (DHA) plasma concentrationC-reactive protein (CRP)

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