CYP2D6

Cytochrome P450, family 2, subfamily D, polypeptide 6
PDB基于2f9q的渲染图
有效结构
PDB 直系同源检索：PDBe, RCSB
PDB查询代码列表

2F9Q, 3QM4, 3TBG, 3TDA, 4WNT, 4WNU, 4WNV, 4WNW

标识
代号 CYP2D6; CPD6; CYP2D; CYP2D7AP; CYP2D7BP; CYP2D7P2; CYP2D8P2; CYP2DL1; CYPIID6; P450-DB1; P450C2D; P450DB1
扩展标识 遗传学：124030 鼠基因：1929474 同源基因：133550 GeneCards: CYP2D6 Gene
EC編號 1.14.14.1
基因本体论描述
分子功能 · monooxygenase activity

· iron ion binding
· drug binding
· arachidonic acid epoxygenase activity
· steroid hydroxylase activity
· oxidoreductase activity
· oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
· oxygen binding
· heme binding

· aromatase activity
细胞成分 · cytoplasm

· mitochondrion
· endoplasmic reticulum

· endoplasmic reticulum membrane
生物过程 · xenobiotic metabolic process

· steroid metabolic process
· coumarin metabolic process
· alkaloid metabolic process
· alkaloid catabolic process
· monoterpenoid metabolic process
· drug metabolic process
· arachidonic acid metabolic process
· isoquinoline alkaloid metabolic process
· drug catabolic process
· exogenous drug catabolic process
· small molecule metabolic process
· heterocycle metabolic process
· negative regulation of binding
· oxidation-reduction process
· oxidative demethylation

· negative regulation of cellular organofluorine metabolic process
Sources: Amigo / QuickGO
RNA表达模式
更多表达数据
直系同源体
物种 人类 小鼠
Entrez 1565 13101
Ensembl ENSG00000100197 ENSMUSG00000094806
UniProt P10635 P24456
mRNA序列 NM_000106 NM_010005
蛋白序列 NP_000097 NP_034135
基因位置 Chr 22:
42.13 – 42.13 Mb		 Chr 15:
82.4 – 82.41 Mb
PubMed查询 [1] [2]
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细胞色素 P450 2D6（cytochrome P450 2D6，CYP2D6）是一种由人类CYP2D6基因编码的酶。CYP2D6主要合成而显现于肝脏，并且也表现在中枢神经系统中，包括黑质。

CYP2D6是细胞色素P450混合功能氧化酶系统的成员之一，是人体中最重要的代谢酶之一。CYP2D6参与25%的临床药物的代谢和清除，过程主要是O-去甲基化。[1]CYP2D6也参与多种内源性物质的代谢，如5-羟色胺和神经类固醇。[1]

引用

  1. ^ 1.0 1.1 Wang B, Yang LP, Zhang XZ, Huang SQ, Bartlam M, Zhou SF. New insights into the structural characteristics and functional relevance of the human cytochrome P450 2D6 enzyme. Drug Metab. Rev. 2009, 41 (4): 573–643. PMID 19645588. doi:10.1080/03602530903118729. 

延伸閱讀

  • Smith G, Stubbins MJ, Harries LW, Wolf CR. Molecular genetics of the human cytochrome P450 monooxygenase superfamily. Xenobiotica. 1998, 28 (12): 1129–65. PMID 9890157. doi:10.1080/004982598238868. 
  • Wolf CR, Smith G. Cytochrome P450 CYP2D6. IARC Sci. Publ. 1999, (148): 209–29. PMID 10493260. 
  • Ding X, Kaminsky LS. Human extrahepatic cytochromes P450: function in xenobiotic metabolism and tissue-selective chemical toxicity in the respiratory and gastrointestinal tracts. Annu. Rev. Pharmacol. Toxicol. 2003, 43 (1): 149–73. PMID 12171978. doi:10.1146/annurev.pharmtox.43.100901.140251. 
  • Lilienfeld S. Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease. CNS Drug Rev. 2002, 8 (2): 159–76. PMID 12177686. doi:10.1111/j.1527-3458.2002.tb00221.x. 
  • Yu AM, Idle JR, Gonzalez FJ. Polymorphic cytochrome P450 2D6: humanized mouse model and endogenous substrates. Drug Metab. Rev. 2004, 36 (2): 243–77. PMID 15237854. doi:10.1081/DMR-120034000. 
  • Abraham JE, Maranian MJ, Driver KE, Platte R, Kalmyrzaev B, Baynes C, Luccarini C, Shah M, Ingle S, Greenberg D, Earl HM, Dunning AM, Pharoah PD, Caldas C. CYP2D6 gene variants: association with breast cancer specific survival in a cohort of breast cancer patients from the United Kingdom treated with adjuvant tamoxifen. Breast Cancer Res. 2010, 12 (4): R64. PMC 2949659 可免费查阅. PMID 20731819. doi:10.1186/bcr2629. 
  • Abraham JE, Maranian MJ, Driver KE, Platte R, Kalmyrzaev B, Baynes C, Luccarini C, Earl HM, Dunning AM, Pharoah PD, Caldas C. CYP2D6 gene variants and their association with breast cancer susceptibility. Cancer Epidemiol. Biomarkers Prev. 2011, 20 (6): 1255–8. PMID 21527579. doi:10.1158/1055-9965.EPI-11-0321. 

外部連結

  • Flockhart Lab Cyp2D6 Substrates Page（页面存档备份，存于互联网档案馆） at IUPUI
  • PharmGKB: Annotated PGx Gene Information for CYP2D6
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双加氧酶（英语：Oxidoreductase）类，包括类固醇羟化酶（英语：steroid hydroxylases）（EC 1.14）
1.14.11（英语：List of EC numbers (EC 1)#EC 1.14.11 With 2-oxoglutarate as one donor.2C and incorporation of one atom each of oxygen into both donors）：以α-酮戊二酸为供体
  • 脯氨酰羟化酶（英语：Prolyl hydroxylase）
  • 赖氨酰羟化酶（英语：Lysyl hydroxylase）
1.14.11：以NADH或NADPH为供体
  • 苯1,2-双加氧酶
  • 5-吡哆酸双加氧酶
  • 邻苯二甲酸1,2-双加氧酶
  • 苯甲酸1,2-双加氧酶
  • 甲苯双加氧酶
  • 萘1,2-双加氧酶
  • 对苯二酸1,2-双加氧酶
  • 一氧化氮双加氧酶
  • 脱镁叶绿酸a加氧酶
  • 苯甲酰辅酶A双加氧酶
  • 咔唑1,9a-双加氧酶
1.14.13（英语：List of EC numbers (EC 1)#EC 1.14.13 With NADH or NADPH as one donor.2C and incorporation of one atom of oxygen）：以NADH或NADPH为供体
  • 含黄素单加氧酶（英语：Flavin-containing monooxygenase）（FMO1（英语：FMO1）、FMO2（英语：FMO2）、FMO3（英语：FMO3）、FMO4（英语：FMO4）、FMO5（英语：FMP5））
  • 一氧化氮合酶（NOS1（英语：NOS1）、NOS2（英语：NOS2）、NOS3（英语：NOS3））
  • 胆固醇7α-羟化酶
  • 甲烷单加氧酶
  • CYP3A4
  • 羊毛固醇14α-脱甲基酶
1.14.14：以还原型黄素黄素或黄素蛋白为供体
1.14.15：以还原型铁硫蛋白为供体
1.14.16：以还原型蝶啶为受体
1.14.17：以还原型抗坏血酸为受体
1.14.18
1.14.19
  • 硬脂酰辅酶A脱饱和酶1
1.14.20：以α-酮戊二酸为受体
1.14.99：杂项
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（英语：Template:Ligases CO CS and CN）/4/5-6