Abstract
[Machine translation] The present invention relates to 4-chloro-3- {[(3-nitrophenyl) amino] sulfonyl} benzoic acid (CNFASB), a specific mitochondrial citrate carrier (CIC) inhibitor. The citrate carrier (CIC) catalyzes the electroneutral exchange between citrate (H-citrate2-) and the unprotonated form of malate (malate2-). The citrate exported from the mitochondria to the cytosol, through the CIC, is cleaved by ATP-citrate lyase (CL) into oxaloacetate and acetylCoA, which will lead to the biosynthesis of sterols and fatty acids. AcetylCoA is necessary for the elongation of polyunsaturated fatty acids that will reform the arachidonic acid used in the biosynthesis of prostaglandins during the inflammatory process. The oxaloacetate produced in the cytosol by CL is reduced to malate, and the latter, in turn, converted into pyruvate by the malic enzyme with the consequent production, in the cytosol, of NADPH+\ H+ necessary for the synthesis of sterols and fatty acids but also for the activity of the enzyme inducible nitric oxide synthase (iNOS) that will produce NO and for the activity of NADPH oxidase that will produce ROS.
| Translated title of the contribution | [Machine translation] citrate carrier inhibitors in the treatment of inflammation |
|---|---|
| Original language | Italian |
| Patent number | RM2013A000167 |
| Publication status | Published - 2013 |
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