11β-羟基类固醇脱氢酶1型

求闻百科，共笔求闻

11β-羟基类固醇脱氢酶1型（HSD11B1），也称为可的松还原酶，是一种NADPH依赖性酶，在包括肝脏、脂肪组织和中枢神经系统在内的关键代谢组织中高度表达。在这些组织中，HSD11B1将可的松还原为激活糖皮质激素受体的活性激素皮质醇。属于短链脱氢酶家族。

功能

这个基因编码的蛋白质是一种微粒体酶，催化应激激素皮质醇转化为非活性代谢物可的松。此外，编码的蛋白质可以催化相反的反应，即可的松转化为皮质醇。过多的皮质醇会导致中枢性肥胖，这种基因的一个特殊变异与儿童肥胖和胰岛素抵抗有关。在这个基因中发现了两个编码相同蛋白质的转录变体。[1]

Cortisol-cortisone equilibrium
Cortisol-cortisone equilibrium

临床意义

11β-HSD1被通常用于治疗消化性溃疡的药物卡宾诺酮抑制。此外，从甘草（glycyrrhiza glabra）根中提取的18α-甘草酸被发现是一种抑制剂。[2]

水杨酸盐下调肥胖小鼠脂肪组织中11β-HSD1的表达，从而解释了阿司匹林改善2型糖尿病血糖控制的原因。[3]绿茶中的表没食子儿茶素没食子酸酯也能有效地抑制这种酶；[4]绿茶是多种酚类物质的复杂混合物，其含量随着生产和加工的不同而变化，其中一些酚类物质是已知的改变遗传表达的HDAC抑制剂。绿茶中的EGCG通常很难被血液吸收。需要更多的研究才能得出明确的结论。[来源请求]

参见

参考文献

  1. ↑ Entrez Gene: HSD11B1 hydroxysteroid (11-beta) dehydrogenase 1. 
  2. ↑ Classen-Houben D, Schuster D, Da Cunha T, Odermatt A, Wolber G, Jordis U, Kueenburg B. Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid. The Journal of Steroid Biochemistry and Molecular Biology. 2009-02, 113 (3–5): 248–52. PMID 19429429. doi:10.1016/j.jsbmb.2009.01.009. 
  3. ↑ Nixon M, Wake DJ, Livingstone DE, Stimson RH, Esteves CL, Seckl JR, Chapman KE, Andrew R, Walker BR. Salicylate downregulates 11β-HSD1 expression in adipose tissue in obese mice and in humans, mediating insulin sensitization. Diabetes. 2012-04, 61 (4): 790–6. PMC 3314355 可免费查阅. PMID 22357964. doi:10.2337/db11-0931. 
  4. ↑ Hintzpeter J, Stapelfeld C, Loerz C, Martin HJ, Maser E. Green tea and one of its constituents, Epigallocatechine-3-gallate, are potent inhibitors of human 11β-hydroxysteroid dehydrogenase type 1. PLoS ONE. 2014-01-03, 9 (1): e84468. Bibcode:2014PLoSO...984468H. PMC 3880318 可免费查阅. PMID 24404164. doi:10.1371/journal.pone.0084468. 

外部链接

拓展阅读

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氧化还原酶：以CH-OH基团为供体的氧化还原酶类（EC 1.1）
1.1.1：以NAD或NADP为受体
醇脱氢酶 · 醛酮还原酶（1A1、1B1、1B10、1C1、1C3、1C4、7A2） · 醛糖还原酶 · 糖类脱氢酶 · 肉碱脱氢酶 · DXP还原异构酶 · 葡萄糖-6-磷酸脱氢酶 · 甘油-3-磷酸脱氢酶 · HMG-CoA还原酶 · 3-羟酰辅酶A脱氢酶 · β-羟基丁酰辅酶A脱氢酶 · 异柠檬酸脱氢酶 · 单磷酸次黄嘌呤核苷酸脱氢酶 · β-酮脂酰-ACP还原酶 · 乳酸盐脱氢酶 · 苹果酸脱氢酶 · 磷酸葡萄糖酸脱氢酶 · L-苏氨酸脱氢酶 · L-木酮糖还原酶 · 山梨醇脱氢酶 · 奎尼酸脱氢酶
羟基类固醇脱氢酶：3-β（3-β-HSD、固醇-4-α-羧酸盐- 3-脱氢酶） · 11-β（11β-羟基类固醇脱氢酶1型、11-β-羟基类固醇脱氢酶2型） · 17-β
1.1.2：以细胞色素为受体
D-乳酸盐脱氢酶 (细胞色素) · D-乳酸盐脱氢酶 (细胞色素c-553) · 甘露醇脱氢酶 (细胞色素)
1.1.3：以 氧气为受体
葡萄糖氧化酶 · L-古洛糖酸内酯氧化酶 · 黄嘌呤氧化酶
1.1.4：以二硫化物为受体
维生素K环氧化物还原酶 · 维生素K环氧化物还原酶 (对华法林不敏感)
1.1.5：以醌类似化合物为受体
醌蛋白葡萄糖脱氢酶
1.1.99：以其他物质为受体
胆碱脱氢酶 · L-2-羟基戊二酸脱氢酶

EC 1.1/2/3/4/5/6/7/8/9/10/11/12/13/14/15/16/17/18/19/20/21/22  · 2.1/2/3/4/5/6/7(2.7.10/11-12)/8/9  · 3.1/2/3/4(3.4.21/22/23/24)/5/6/7/8/9/10/11/12/13  · 4.1/2/3/4/5/6 · 5.1/2/3/4/5/99 · |6.1-3/4/5-6

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