Fatty acid-binding proteins (FABPs) are members of the intracellular lipid-binding protein (iLBP) family and are involved in reversibly binding intracellular hydrophobic ligands and trafficking them throughout cellular compartments, including the peroxisomes, mitochondria, endoplasmic reticulum and nucleus. FABPs are small, structurally conserved cytosolic proteins consisting of a water-filled, interior-binding pocket surrounded by ten anti-parallel beta sheets, forming a beta barrel. At the superior surface, two alpha-helices cap the pocket and are thought to regulate binding. FABPs have broad specificity, including the ability to bind long-chain (C16-C20) fatty acids, eicosanoids, bile salts and peroxisome proliferators.
FABPs are ubiquitously expressed throughout tissues that are highly active in FA metabolism and comprise several isoforms. To date, nine FABP protein-coding genes have been identified in the human genome. These include liver (L-FABP), intestine- (I-FABP), heart- (H-FABP), adipocyte- (A-FABP), epidermal- (E-FABP), ileal- (Il-FABP), brain- (B-FABP), myelin- (M-FABP) and testis-FABP (T-FABP).
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A potent, selective, cell-permeable and orally active inhibitor of FABP4 (Fatty acid binding protein 4) with Ki of < 2 nM; improves endothelial function, phosphorylated and total eNOS and reduces plasma triglyceride levels but does not affect endothelium-independent relaxations in mice; exhibits an effective therapeutic activity against severe atherosclerosis and type 2 diabetes in mouse models.
FABP4 inhibitor 1
A potent, selective FABP4 inhibitor with Ki of 30 nM.
SBFI-26 (SBFI26) is a small molecule inhibitor of epidermal- and brain-specific FABP5 and FABP7 that effectively increases anandamide signaling; dose-dependently reduces mechanical hyperalgesia in vivo, demonstrates significant analgesic and anti-inflammatory properties; also suppresses the malignant progression of castration resistant prostate cancer cells by competitively binding to oncogenic FABP5.
HTS01037 is a highly potent ligand of adipocyte fatty acid binding protein (A-FABP/aP2) with Ki of 0.67 uM; competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2, antagonizes the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes at 10 uM; inhibits lipolysis in 3T3L1 adipocytes and reduces lipopolysaccharide-stimulated inflammation in bone marrow-derived macrophages.
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