Lipofermata (297180-15-5) is an inhibitor of fatty acid transport protein 2 (FATP2; IC50?= 4.84 μM).1?It does not inhibit glucose transport or the activity of long chain acyl-CoA synthetase. It prevented palmitate-mediated oxidative stress, induction of BiP and CHOP, and cell death in a dose-dependent manner in hsHepG2 and mINS-1E cells suggesting utility in preventing fatty acid-mediated cell death pathways and lipotoxic disease.2?Inhibition was specific for long and very long chain fatty acids but not medium (C6-C10) acids. Lipofermata abrogates lipid transport into melanoma cells and reduces melanoma growth and invasion.3
Lipofermata is a fatty acid transport proteins (FATPs) inhibitor.
1) Sandoval?et al.?(2010),?Identification and characterization of small compound inhibitors of human FATP2; Biochem. Pharmacol.?79?990
2) Ahowesso?et al.?(2015),?Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death; Biochem. Pharmacol.?98?167
3) Zhang?et al.?(2018),?Adipocyte-derived lipids mediate melanoma progression via FATP proteins; Cancer Discov.?8?1006
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