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1
Selective inhibition of cholesterol synthesis by cell-free preparations of rat liver by using inhibitors of cytoplasmic acetoacetyl-coenzyme A thiolase.利用细胞质乙酰乙酰辅酶A硫解酶抑制剂，通过大鼠肝脏无细胞制剂选择性抑制胆固醇合成。
Biochem J. 1975 Jun;147(3):531-9. doi: 10.1042/bj1470531.
2
Synthesis of chloromethyl ketone derivatives of fatty acids. Their use as specific inhibitors of acetoacetyl-coenzyme A thiolase, cholesterol biosynthesis and fatty acid synthesis.脂肪酸氯甲基酮衍生物的合成。它们作为乙酰乙酰辅酶A硫解酶、胆固醇生物合成和脂肪酸合成的特异性抑制剂的用途。
Biochem J. 1978 Dec 1;175(3):999-1011. doi: 10.1042/bj1750999.
3
The inhibition of cytoplasmic acetoacetyl-CoA thiolase by a triyne carbonate (L-660, 631).三炔碳酸酯（L-660, 631）对细胞质乙酰乙酰辅酶A硫解酶的抑制作用
Biochem Biophys Res Commun. 1989 Aug 30;163(1):548-53. doi: 10.1016/0006-291x(89)92172-4.
4
The kinetic mechanism and properties of the cytoplasmic acetoacetyl-coenzyme A thiolase from rat liver.大鼠肝脏细胞质乙酰乙酰辅酶A硫解酶的动力学机制及特性
Biochem J. 1974 Apr;139(1):109-21. doi: 10.1042/bj1390109.
5
Rat liver peroxisomes catalyze the initial step in cholesterol synthesis. The condensation of acetyl-CoA units into acetoacetyl-CoA.大鼠肝脏过氧化物酶体催化胆固醇合成的起始步骤。即乙酰辅酶A单位缩合形成乙酰乙酰辅酶A。
J Biol Chem. 1990 Apr 5;265(10):5731-5.
6
Regulation of hepatic cholesterol biosynthesis by fatty acids: effect of feeding olive oil on cytoplasmic acetoacetyl-coenzyme A thiolase, beta-hydroxy-beta-methylglutaryl-CoA synthase, and acetoacetyl-coenzyme A ligase.脂肪酸对肝脏胆固醇生物合成的调节：喂食橄榄油对细胞质乙酰乙酰辅酶A硫解酶、β-羟基-β-甲基戊二酰辅酶A合酶和乙酰乙酰辅酶A连接酶的影响。
Biochem Biophys Res Commun. 1988 May 31;153(1):422-7. doi: 10.1016/s0006-291x(88)81241-5.
7
Mechanism of action of beta-oxoacyl-CoA thiolase from rat liver cytosol. Direct evidence for the order of addition of the two acetyl-CoA molecules during the formation of acetoacetyl-CoA.大鼠肝脏胞质溶胶中β-氧代酰基辅酶A硫解酶的作用机制。在乙酰乙酰辅酶A形成过程中两个乙酰辅酶A分子添加顺序的直接证据。
Biochem J. 1983 Jul 1;213(1):153-8. doi: 10.1042/bj2130153.
8
Regulation of early cholesterol biosynthesis in rat liver: effects of sterols, bile acids, lovastatin, and BM 15.766 on 3-hydroxy-3-methylglutaryl coenzyme A synthase and acetoacetyl coenzyme A thiolase activities.大鼠肝脏早期胆固醇生物合成的调节：固醇、胆汁酸、洛伐他汀和BM 15.766对3-羟基-3-甲基戊二酰辅酶A合酶和乙酰乙酰辅酶A硫解酶活性的影响。
Hepatology. 1998 Jan;27(1):154-9. doi: 10.1002/hep.510270124.
9
Inhibition of sterol synthesis by citrinin in a cell-free system from rat liver and yeast.桔霉素在大鼠肝脏和酵母的无细胞体系中对固醇合成的抑制作用。
Biochim Biophys Acta. 1977 Feb 23;486(2):254-9.
10
On the mechanism of ketogenesis and its control. Purification, kinetic mechanism and regulation of different forms of mitochondrial acetoacetyl-CoA thiolases from ox liver.关于生酮作用的机制及其调控。牛肝中不同形式的线粒体乙酰乙酰辅酶A硫解酶的纯化、动力学机制及调控
Eur J Biochem. 1975 Nov 15;59(2):475-89. doi: 10.1111/j.1432-1033.1975.tb02476.x.

引用本文的文献

1
Effect of methyl 2-hexadecynoate on hepatic fatty acid metabolism.2-十六碳炔酸甲酯对肝脏脂肪酸代谢的影响。
Lipids. 1980 Mar;15(3):141-50. doi: 10.1007/BF02540960.
2
Synthesis of chloromethyl ketone derivatives of fatty acids. Their use as specific inhibitors of acetoacetyl-coenzyme A thiolase, cholesterol biosynthesis and fatty acid synthesis.脂肪酸氯甲基酮衍生物的合成。它们作为乙酰乙酰辅酶A硫解酶、胆固醇生物合成和脂肪酸合成的特异性抑制剂的用途。
Biochem J. 1978 Dec 1;175(3):999-1011. doi: 10.1042/bj1750999.

本文引用的文献

1
Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase.甲磺酸酯作为乙酰胆碱酯酶的不可逆抑制剂
J Biol Chem. 1962 Oct;237:3245-9.
2
The participation of malonyl coenzyme A in the biosynthesis of mevalonic acid.丙二酰辅酶A在甲羟戊酸生物合成中的参与。
J Biol Chem. 1963 Apr;238:1294-301.
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Desmosterol deposition in human and experimental atherosclerosis.
Circ Res. 1963 Feb;12:228-34. doi: 10.1161/01.res.12.2.228.
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beta-Hydroxy-beta-methyl-glutaryl coenzyme A reductase, cleavage and condensing enzymes in relation to cholesterol formation in rat liver.β-羟基-β-甲基戊二酰辅酶A还原酶、裂解酶和缩合酶与大鼠肝脏胆固醇形成的关系
Biochim Biophys Acta. 1960 Jun 3;40:491-501. doi: 10.1016/0006-3002(60)91390-1.
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Tissue sulfhydryl groups.组织巯基
Arch Biochem Biophys. 1959 May;82(1):70-7. doi: 10.1016/0003-9861(59)90090-6.
6
Functional group of coenzyme A and its metabolic relations, especially in the fatty acid cycle.辅酶A的功能基团及其代谢关系，尤其是在脂肪酸循环中的代谢关系。
Fed Proc. 1953 Sep;12(3):683-91.
7
Enzymatic synthesis of the coenzyme A derivatives of long chain fatty acids.长链脂肪酸辅酶A衍生物的酶促合成。
J Biol Chem. 1953 Sep;204(1):329-43.
8
Assay of the mycobactins by measurement of the growth of Mycobacterium johnei.通过测量副结核分枝杆菌的生长来测定分枝杆菌素。
Biochem J. 1966 Jul;100(1):47-9. doi: 10.1042/bj1000047.
9
The status of C-6, C-7, C-15 and C-16 hydrogen atoms in cholesterol biosynthesis.胆固醇生物合成中C-6、C-7、C-15和C-16氢原子的状态。
Eur J Biochem. 1969 May 1;9(1):107-11. doi: 10.1111/j.1432-1033.1969.tb00582.x.
10
The reaction of fumarase with iodoacetate and 4-bromocrotonate.延胡索酸酶与碘乙酸盐和4-溴巴豆酸盐的反应。
J Biol Chem. 1969 Apr 10;244(7):1755-63.

利用细胞质乙酰乙酰辅酶A硫解酶抑制剂，通过大鼠肝脏无细胞制剂选择性抑制胆固醇合成。

Selective inhibition of cholesterol synthesis by cell-free preparations of rat liver by using inhibitors of cytoplasmic acetoacetyl-coenzyme A thiolase.

作者信息

Bloxham D P

出版信息

Biochem J. 1975 Jun;147(3):531-9. doi: 10.1042/bj1470531.

DOI:10.1042/bj1470531
PMID:241330
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1165481/
Abstract

Cytoplasmic acetoacetyl-CoA thiolase (acetyl-CoA C-acetyltransferase, EC 2.3.1.9) was partially purified from rat liver. The enzyme was irreversibly inactivated by 4-bromocrotonyl-CoA, but-3-ynoyl-CoA, pent-3-ynoyl-CoA and dec-3-ynoyl-CoA. In the case of the alk-3-ynoyl-CoA esters the potency as alkylating agents of acetoacetyl-CoA thiolase decreased with increased chain length of the alk-3-ynoyl moiety. Advantage was taken of the specific action of alk-3-ynoyl-CoA esters on acetoacetyl-CoA thiolase to show that in a postmitochondrial fraction from rat liver they are effective inhibitors of cholesterol synthesis from sodium [2-14C]acetate under conditions when mevalonate conversion into cholesterol and fatty acid synthesis are unafffected. Short-chain alk-3-ynoic acids have little effect on sterol synthesis, although dec-3-ynoic acid is an effective inhibitor owing to its conversion into the CoA ester by the microsomal fatty acyl-CoA synthetase.

摘要

从大鼠肝脏中部分纯化了细胞质乙酰乙酰辅酶A硫解酶（乙酰辅酶A C - 乙酰转移酶，EC 2.3.1.9）。该酶可被4 - 溴巴豆酰辅酶A、丁 - 3 - 炔酰辅酶A、戊 - 3 - 炔酰辅酶A和癸 - 3 - 炔酰辅酶A不可逆地失活。对于3 - 炔酰辅酶A酯，随着3 - 炔酰部分链长的增加，乙酰乙酰辅酶A硫解酶作为烷基化剂的效力降低。利用3 - 炔酰辅酶A酯对乙酰乙酰辅酶A硫解酶的特异性作用表明，在大鼠肝脏的线粒体后组分中，在甲羟戊酸转化为胆固醇和脂肪酸合成不受影响的条件下，它们是[2 - 14C]乙酸钠合成胆固醇的有效抑制剂。短链3 - 炔酸对甾醇合成影响很小，尽管癸 - 3 - 炔酸由于其被微粒体脂肪酰辅酶A合成酶转化为辅酶A酯而成为有效抑制剂。