acyl-coenzyme

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active, selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) with an EC50 of 9 nM.

Acyl coenzyme A synthetase (ACS), also known as acetyl coenzyme A synthetase, catalyzes the activation of fatty acids via coenzyme A through a two-step thioesterification process, forming acyl coenzyme A. It is crucial in anabolic and catabolic lipid metabolism pathways and contributes to the tricarboxylic acid (TCA) cycle during aerobic respiration [1].

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT), useful for studying high-lipid-related diseases.

Eflucimibe (L0081) is an acyl coenzyme A: cholesterol acyltransferase inhibitor for the treatment of cardiovascular disease and endocrine and metabolic disorders, and can be used to study atherosclerosis and hyperlipidemia.

CL 277082 (Ddpmhu) is an acyl coenzyme A:cholesterol O-acyltransferase inhibitor that inhibits granuloma tissue ACAT activity.

Increased levels of erucic acid (22:1n9) have been found in the red blood cell membranes of autistic subjects with developmental regression (PMID: 16581239 ). Erucic acid (13(Z)-Docosenoic Acid) is broken down long-chain acyl-coenzyme A (CoA) dehydrogenase, which is produced in the liver. This enzyme breaks this long chain fatty acid into shorter-chain fatty acids. human infants have relatively low amounts of this enzyme and because of this, babies should not be given foods high in erucic acid. Erucic acid is found to be associated with isovaleric acidemia, which is an inborn error of metabolism.

2-Hydroxyoctanoic acid is a medium-chain acyl-coenzyme A synthetase inhibitor (Ki:500 μM). 3-Hydroxymandelic acid is a protein hydrolysis product of larger proteins.

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg kg) reduces the size of aortic atherosclerotic lesions inLdlr- -andApoE- -mouse models of atherosclerosis. 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Coenzyme A is an obligatory cofactor in all living cells synthesized from pantothenate (Vitamin B5), adenosine triphosphate (ATP), and cysteine.

Nevanimibe is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).

Pyripyropene A is a potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2) acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) with an IC50 of 0.07 μM.

Triacsin C (WS 1228A) from Streptomyces aureofaciens is a differential inhibitor of arachidonic acid coenzyme A synthetase and non-specific long-chain acyl-coenzyme A synthetase, with anti-atherosclerotic activity, inhibition of ACSL activity, and inhibition of the accumulation of TAGs into lipid droplets (LDs).Triacsin C has been used to study rotavirus infection and Alzheimer;s disease. Triacsin C is used to study rotavirus infection and Alzheimer;s disease.

Pentanoyl Coenzyme A (pentanoyl-CoA) Free acid is a short-chain acyl-CoA. It acts as a metabolite of 3-oxopropionyl-CoA.

YM-750 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC50 value of 0.18 μM. ACAT is an enzyme that catalyzes the conversion of cholesterol and long-chain fatty-acyl-coenzyme A into cholesteryl esters.

Avasimibe (PD-148515) is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the arterial wall. It also inhibits human P450 isoenzymes CYP2C9/1A2/2C19 (IC50: 2.9/13.9/26.5 μM).

Lauroyl-coenzyme A can function as an acyl group carrier, acetyl-CoA. It can be used as an intermediate in lipid metabolism and is involved in lipid biosynthesis and fatty acid transport.

Linoleoyl-coenzyme A is a substrate used to investigate the specificity and kinetics of acyl-CoA.

Acyl-coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).

Acyl-Coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM.

Terpendole C is an indole diterpene alkaloid fungal metabolite originally isolated from A. yamanashiensis and an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 2.1 μM in rat liver microsomes). It also inhibits ACAT in J774 macrophages (IC50 = 0.46 μM) without affecting cell growth.

Isobutyryl coenzyme A (isobutyryl-CoA) is a short-chain branched acyl CoA. Isobutyryl-CoA is a substrate for isobutyryl-CoA dehydrogenase (IBDH) in the catabolism of valine and an intermediate in the synthesis of isobutyryl-L-carnitine , which accumulates in IBDH deficiency.

Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.