Target intelligence / Profile preview

Fatty acid-binding proteins (FABP)

Target
FABP
Molecular classification
Lipid-binding protein, Intracellular lipid-binding protein (iLBP), Transporter (internal, not membrane transporter)
01

Overview

Fatty acid-binding proteins (FABPs) form a conserved family of small (∼14-15 kDa) intracellular proteins, each with tissue-specific expression that reflects their specialized roles in lipid handling. FABPs bind long-chain fatty acids and related hydrophobic molecules with high affinity, facilitating their solubilization and transport to various compartments (nucleus, mitochondria, endoplasmic reticulum). They enable efficient intracellular trafficking of fatty acids for metabolism, storage, and signaling. Individual FABP subtypes are highly conserved across species and are central to systemic lipid metabolism, gene expression regulation, immune response, and cellular stress adaptation. FABPs have gained substantial interest as both diagnostic biomarkers (indicative of tissue injury or disease) and therapeutic targets for disorders ranging from diabetes and cardiovascular disease to some cancers and inflammatory conditions.

Other names
Liver-type fatty acid-binding protein (L-FABP, FABP1)Adipocyte fatty acid-binding protein (A-FABP, FABP4)Intestinal fatty acid-binding protein (I-FABP, FABP2)Heart-type fatty acid-binding protein (H-FABP, FABP3)Epidermal fatty acid-binding protein (E-FABP, FABP5)lipid chaperonefatty acid transporter
02

Mechanism of action

Inhibition of fatty acid binding/transport Modulation of lipid signaling pathways Regulation of gene expression through altered lipid trafficking Some drugs act as competitive inhibitors of the FABP binding site

03

Biological functions

Fatty acid binding and solubilizationIntracellular transport of fatty acids and other hydrophobic lipidsLipid metabolism and homeostasisModulation of gene expression via lipid signalingAdipogenesis (fat cell differentiation)Cell proliferation, apoptosis, and immune response regulationAntioxidant activity
04

Disease associations

Metabolic diseases (obesity, diabetes, metabolic syndrome)Cardiovascular disease (atherosclerosis)Cancer (certain FABPs in tumorigenesis)InflammationSkin diseases, neurological diseases (e.g., FABP5 functions)Other: liver diseases, tissue injury
05

Safety considerations

Potential effects on systemic energy homeostasis if multiple FABPs are inhibitedRisk of metabolic disturbances or unintended immune effects, particularly if tissue-specific selectivity is lacking
06

Interacting drugs

BMS309403 (FABP4 inhibitor)

2 more in the full profile.

07

Biomarkers

Serum/plasma levels of heart-type FABP (FABP3) as biomarkers for myocardial injurySerum adipocyte FABP (FABP4) associated with metabolic syndrome and obesityFABP1 and FABP2 as markers for liver and intestinal injury

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