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CPT-I inhibitors: etomoxir, oxfenicine, perhexiline CPT-I (carnitine palmitoyl transferase) converts fatty acyl-CoA to fatty acyl-carnitine. Carnitine biosynthesis inhibitor: mildronate [1] 3-KAT inhibitors: trimetazidine 3-KAT (3-ketoacyl-coenzyme A thiolase) inhibitors directly inhibits fatty acid beta-oxidation.
Overview of the synthase cycle: (1) Activation (apo→holo) of the FAS by ACPS, (2) priming with Acetyl-CoA by AT, (3) transfer of the acetyl group from the ACP to the active site of the KS, (4) transacylation of the ACP with Maloyl-CoA by MPT, Claisen condensation at the KS by (5) decarboxylation and (6) nucleophilic attack of the enolate at ...
Lipogenesis inhibitor is a class of drug that works by inhibiting de novo lipogenesis—the generation of fatty acids in the body. These drugs target enzymes involved in lipogenesis, such as citrate/isocitrate carrier (CIC), ATP-citrate lyase (ACLY), acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS).
Carnitine palmitoyltransferase I (CPT1) also known as carnitine acyltransferase I, CPTI, CAT1, CoA:carnitine acyl transferase (CCAT), or palmitoylCoA transferase I, is a mitochondrial enzyme responsible for the formation of acyl carnitines by catalyzing the transfer of the acyl group of a long-chain fatty acyl-CoA from coenzyme A to l-carnitine.
New effective drugs are needed to combat this disease. Inhibitors against mtFabH, or against other enzymes of the FAS-II pathway, may have broader utility, such as the treatment of multidrug-resistant Staphylococcus aureus, and Plasmodium falciparum, the causative agent of another serious refractory problem, malaria.
The latter conversion is mediated by acyl-CoA synthase" acyl-P + HS-CoA → acyl-S-CoA + P i + H + Three types of acyl-CoA synthases are employed, depending on the chain length of the fatty acid. [3] For example, the substrates for medium chain acyl-CoA synthase are 4-11 carbon fatty acids. [4] The enzyme acyl-CoA thioesterase takes of the acyl ...
ACC is a biotin-containing enzyme which catalyzes the carboxylation of acetyl-CoA to malonyl-CoA, the rate-limiting step in fatty acid synthesis. ACC-beta is thought to control fatty acid oxidation by means of the ability of malonyl-CoA to inhibit carnitine palmitoyltransferase I , the rate-limiting step in fatty acid uptake and oxidation by ...
Cerulenin is an antifungal antibiotic that inhibits fatty acid and steroid biosynthesis.It was the first natural product antibiotic known to inhibit lipid synthesis. [1] In fatty acid synthesis, it has been reported to bind in equimolar ratio to b-keto-acyl-ACP synthase, one of the seven moieties of fatty acid synthase, blocking the interaction of malonyl-CoA.