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Potent FTO (fat mass and obesity-associated gene) inhibitor for in vivo studies. FTO belongs to the Fe2+ and α-ketoglutarate (α-KG)-dependent oxygenase family. It demethylates N6-adenosine-modified (m6A) sites and N6,2'-O-dimethyladenosine-modified (m6Am) sites of mRNA. With its demethylase activity, FTO regulates the expression of some uncharacterized genes. The transcription factor FOXO1 has been shown to be a substrate of FTO. FTO demethylated m6A sites on forkhead box protein O1 (FOXO1) mRNA to up-regulate FOXO1 expression, thereby modulating gluconeogenesis and thermogenesis explaining in part the function of FTO on metabolic disorders such as obesity and diabetes.
Potent selective and reversible catechol-O-methyltransferase (COMT) inhibitor, an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Entacapone is selective for COMT over monoamine oxidase A (MAO-A) and MAO-B and phenolsulphotransferase M (PST-M) and PST-P (IC50s = >50 µM). It is used for the treatment of Parkinson’s disease, administered concomittantly with levodopa and a decarboxylase inhibitor (e.g. carbidopa).
Inhibits α-synuclein aggregation in an in vitro assay and blocks α-synuclein-induced cell death in PC-12 cells.
Shown to uncouple oxidative phosphorylation and inhibit mitochondrial enzyme complexes I and IV.
Antioxidant that can scavenge toxic HOCl and ONOO--species and inhibit oxidative stress-induced cell death.
Product References
Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone: E. Nissinen, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 346, 262 (1992)
Different in vivo properties of three new inhibitors of catechol O-methyltransferase in the rat: P.T. Mannisto, et al.; Br. J. Pharmacol. 105, 569 (1992)
The effect of entacapone (OR-611) on brain [18F]-6-L-fluorodopa metabolism: implications for levodopa therapy of Parkinson's disease: G.V. Sawle, et al.; Neurology 44, 1292 (1994)
Entacapone, a novel catechol-O-methyltransferase inhibitor for Parkinson's disease, does not impair mitochondrial energy production: E. Nissinen, et al.; Eur. J. Pharmacol. 340, 287 (1997)
Entacapone. A review of its use in Parkinson's disease: K.J. Holm & C.M. Spencer; Drugs 58, 159 (1999)
Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity: S. Di Giovanni, et al.; J. Biol. Chem. 285, 14941 (2010)
Entacapone is an Antioxidant More Potent than Vitamin C and Vitamin E for Scavenging of Hypochlorous Acid and Peroxynitrite, and the Inhibition of Oxidative Stress-Induced Cell Death: A.Y. Chen, et al.; Med. Sci. Monit. 22, 687 (2016)
The catechol-O-methyltransferase inhibitors tolcapone and entacapone uncouple and inhibit the mitochondrial respiratory chain in HepaRG cells: D. Grunig, et al.; Toxicol. In Vitro 42, 337 (2017)
Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1: S. Peng, et al.; Sci. Transl. Med. 11, eaau7116 (2019)
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