Fatty acid-binding proteins are low molecular weight (100-130 aa) chaperones for long chain fatty acids, fatty acyl CoA esters, eicosanoids, retinols, retinoic acids and related metabolites and are usually regarded as being responsible for allowing the otherwise hydrophobic ligands to be mobile in aqueous media. These binding proteins may perform functions extracellularly (e.g. in plasma) or transport these agents; to the nucleus to interact with nuclear receptors (principally PPARs and retinoic acid receptors [13]) or for interaction with metabolic enzymes. Although sequence homology is limited, crystallographic studies suggest conserved 3D structures across the group of binding proteins.

Although not tested at all FABPs, BMS309403 exhibits high affinity for FABP4 (pIC50 ~8.8) compared to FABP3 or FABP5 (pIC50 <6.6) [4,14]. HTS01037 is reported to interfere with FABP4 action [5]. Ibuprofen displays some selectivity for FABP4 (pIC₅₀ 5.5) relative to FABP3 (pIC₅₀ 3.5) and FABP5 (pIC₅₀ 3.8) [8]. Fenofibric acid displays some selectivity for FABP5 (pIC₅₀ 5.5) relative to FABP3 (pIC₅₀ 4.5) and FABP4 (pIC₅₀ 4.6) [8]. Multiple pseudogenes for the FABPs have been identified in the human genome.

* Key recommended reading is highlighted with an asterisk

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Furuhashi M, Hotamisligil GS. (2008) Fatty acid-binding proteins: role in metabolic diseases and potential as drug targets. Nat Rev Drug Discov, 7 (6): 489-503. [PMID:18511927]

* Gajda AM, Storch J. (2015) Enterocyte fatty acid-binding proteins (FABPs): different functions of liver and intestinal FABPs in the intestine. Prostaglandins Leukot Essent Fatty Acids, 93: 9-16. [PMID:25458898]

* Glatz JF. (2015) Lipids and lipid binding proteins: a perfect match. Prostaglandins Leukot Essent Fatty Acids, 93: 45-9. [PMID:25154384]

* Hotamisligil GS, Bernlohr DA. (2015) Metabolic functions of FABPs--mechanisms and therapeutic implications. Nat Rev Endocrinol, 11 (10): 592-605. [PMID:26260145]

Kralisch S, Fasshauer M. (2013) Adipocyte fatty acid binding protein: a novel adipokine involved in the pathogenesis of metabolic and vascular disease?. Diabetologia, 56 (1): 10-21. [PMID:23052058]

* Matsumata M, Inada H, Osumi N. (2016) Fatty acid binding proteins and the nervous system: Their impact on mental conditions. Neurosci Res, 102: 47-55. [PMID:25205626]

* Nguyen HC, Qadura M, Singh KK. (2020) Role of the Fatty Acid Binding Proteins in Cardiovascular Diseases: A Systematic Review. J Clin Med, 9 (11). DOI: 10.3390/jcm9113390 [PMID:33105856]

* Osumi T, Kuramoto K. (2016) Heart lipid droplets and lipid droplet-binding proteins: Biochemistry, physiology, and pathology. Exp Cell Res, 340 (2): 198-204. [PMID:26524506]

Schroeder F, Petrescu AD, Huang H, Atshaves BP, McIntosh AL, Martin GG, Hostetler HA, Vespa A, Landrock D, Landrock KK et al.. (2008) Role of fatty acid binding proteins and long chain fatty acids in modulating nuclear receptors and gene transcription. Lipids, 43 (1): 1-17. [PMID:17882463]

Storch J, Thumser AE. (2010) Tissue-specific functions in the fatty acid-binding protein family. J Biol Chem, 285 (43): 32679-83. [PMID:20716527]

Yamamoto T, Yamamoto A, Watanabe M, Matsuo T, Yamazaki N, Kataoka M, Terada H, Shinohara Y. (2009) Classification of FABP isoforms and tissues based on quantitative evaluation of transcript levels of these isoforms in various rat tissues. Biotechnol Lett, 31 (11): 1695-701. [PMID:19565192]

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