CYP2D6タンパク質

関: cytochrome P-450 CYP2D6

cytochrome P-450 CYP2D6

同: cytochrome C450 2D6

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/05/18 08:42:22」(JST)

^[1] Cytochrome P450 2D6 (CYP2D6), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. Also, many substances are bioactivated by CYP2D6 to form their active compounds. While CYP2D6 is involved in the oxidation of a wide range of substrates of all the CYPs, there is considerable variability in its expression in the liver. The gene is located near two cytochrome P450 pseudogenes on chromosome 22q13.1. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.^[2]

Genotype/phenotype variability

CYP2D6 shows the largest phenotypical variability among the CYPs, largely due to genetic polymorphism. The genotype accounts for normal, reduced, and non-existent CYP2D6 function in subjects.

The CYP2D6 function in any particular subject may be described as one of the following:

poor metaboliser–these subjects have little or no CYP2D6 function
intermediate metabolizers–these subjects metabolize drugs at a rate somewhere between the poor and extensive metabolizers
extensive metaboliser–these subjects have normal CYP2D6 function
ultrarapid metaboliser–these subjects have multiple copies of the CYP2D6 gene expressed, and therefore greater-than-normal CYP2D6 function

A patient's CYP2D6 phenotype is often clinically determined via the administration of debrisoquine (a selective CYP2D6 substrate) and subsequent plasma concentration assay of the debrisoquine metabolite (4-hydroxydebrisoquine). More recently, a "DNA microarray" has been developed, known as the AmpliChip, which allows the automated determination of a patient's CYP2D6 (and CYP2C19) genotype.

CYP2D6 activity was tested in "healthy infants receiving an oral dose (0.3 mg/kg) of dextromethorphan (DM) at 0.5, 1, 2, 4, 6, and 12 months of age. DM and its major metabolites were measured in urine. CYP2D6 genotype was determined by polymerase chain reaction-restriction fragment length polymorphism. Genotyping data indicated a strong correlation between CYP2D6 genotype and DM O-demethylation (beta=-0.638; 95% CI: -0.745, -0.532; P<0.001). CYP2D6 activity was detectable and concordant with genotype by 2 weeks of age, showed no relationship with gestational age, and did not change with post natal age up to 1 year. In contrast, DM N-demethylation developed significantly more slowly over the first year of life. Genotype and the temporal acquisition of drug biotransformation are critical determinants of a drug response in infants."^[3]

The type of CYP2D6 function of an individual may influence the person's response to different doses of drugs that CYP2D6 metabolizes. The nature of the effect on the drug response depends not only on the type of CYP2D6 function, but also on the extent to which processing of the drug by CYP2D6 results in a chemical that has an effect that is similar, stronger, or weaker than the original drug, or no effect at all. For example, if CYP2D6 converts a drug that has a strong effect into a substance that has a weaker effect, than poor metabolizers (weak CYP2D6 function) will have an exaggerated response to the drug and stronger side-effects; conversely, if CYP2D6 converts a different drug into a substance that has a greater effect than its parent chemical, then extensive metabolizers (strong CYP2D6 function) will have an exaggerated response to the drug and stronger side-effects.^[4]

Genetic basis of variability

The genetic basis for extensive and poor metaboliser variability is the CYP2D6 allele, located on chromosome 22. Subjects possessing certain allelic variants will show normal, decreased, or no CYP2D6 function, depending on the allele.

CYP2D6 allele and enzyme activity^[5]
Allele	CYP2D6 activity
CYP2D61*	normal
CYP2D62*	increased
CYP2D63*	none
CYP2D64*	none
CYP2D65*	none
CYP2D69*	decreased
CYP2D610*	decreased
CYP2D617*	decreased

Ethnic factors in variability

Ethnicity is a factor in the occurrence of CYP2D6 variability. The prevalence of CYP2D6 poor metabolizers is approximately 6–10% in white populations, but is lower in most other ethnic groups such as Asians (2%).^[6] In blacks, the frequency of poor metabolizers is greater than for whites.^[7] The occurrence of CYP2D6 ultrarapid metabolisers appears to be greater among Middle Eastern and North African populations.^[8]

This variability is accounted for by the differences in the prevalence of various CYP2D6 alleles among the populations–approximately 10% of whites appear to have the non-functional CYP2D6*4 allele,^[5] while approximately 50% of Asians possess the CYP2D6*10 allele,^[5] which should produce decreased CYP2D6 function; however this still appears to be within the normal range and are still grouped as intermediate metabolisers.

CYP2D6 ligands

Following is a table of selected substrates, inducers and inhibitors of CYP2D6. Where classes of agents are listed, there may be exceptions within the class.

Inhibitors of CYP2D6 can be classified by their potency, such as:

Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.^[9]
Moderate inhibitor being one that causes at least a 2-fold increase in the plasma AUC values, or 50-80% decrease in clearance.^[9]
Weak inhibitor being one that causes at least a 1.25-fold but less than 2-fold increase in the plasma AUC values, or 20-50% decrease in clearance.^[9]

**Selected inducers, inhibitors and substrates of CYP2D6**
Substrates ↑ = bioactivation by CYP2D6	Inhibitors	Inducers
All^[10] tricyclic antidepressants, e.g. imipramine^[9] amitriptyline^[9] etc. Most^[10] SSRIs (antidepressant), e.g. fluoxetine^[9] paroxetine^[9] fluvoxamine^[9] venlafaxine^[9]^[10] (SNRI antidepressant) mianserin^[10] (tetracyclic antidepressant) opioids codeine^[9]^[10] ↑^[11] into morphine tramadol^[9]^[10] ↑^[11] oxycodone ^[9] antipsychotics, e.g. haloperidol^[9]^[10] risperidone^[9]^[10] perphenazine^[9]^[10] thioridazine^[9]^[10] zuclopenthixol^[9]^[10] iloperidone^[9]^[10] aripiprazole^[9]^[10] chlorpromazine^[9]^[10] levomepromazine^[10] remoxipride^[10] minaprine^[9] (RIMA antidepressant) tamoxifen^[9]^[10] ↑^[12] (SERM) beta-blockers metoprolol^[9]^[10] timolol^[9]^[10] alprenolol^[9]^[10] carvedilol^[9] bufuralol^[9] nebivolol^[9] propranolol^[9] debrisoquine^[9] (antihypertensive) Class I antiarrhythmics flecainide^[9]^[10] propafenone^[9]^[10] encainide^[9]^[10] mexiletine^[9]^[10] lidocaine^[9] sparteine^[9] ondansetron^[9]^[10] (antiemetic) donepezil^[9]^[10] (acetylcholinesterase inhibitor) phenformin^[9]^[10] (antidiabetic) tropisetron^[10] (5-HT3 receptor antagonist) amphetamine^[9] (in ADHD, narcolepsy) atomoxetine^[9] (in ADHD) chlorphenamine^[9] (antihistamine) dexfenfluramine^[9] (serotoninergic anorectic) dextromethorphan^[9] (antitussive) into psychoactive dextrorphan duloxetine^[9] (SNRI) metoclopramide^[9] (dopamine antagonist) Methoxyamphetamine^[9] perhexiline^[9] (antianginal agent) phenacetin^[9] (analgesic) promethazine^[9] (antihistamine antiemetic)	strong: SSRIs fluoxetine^[9]^[10] paroxetine^[9]^[10] bupropion^[9] (non-SSRI antidepressant) quinidine^[9]^[10] (class I antiarrhythmic agent) cinacalcet^[9] (calcimimetic) ritonavir^[10] (antiretroviral) Moderate sertraline^[9] (SSRI) duloxetine^[9] (SNRI terbinafine^[9] (antifungal) weak: buprenorphine^[13] (in opioid addiction) amiodarone^[9] (antiarrhythmic) cimetidine^[9] (H2-receptor antagonist) unspecified potency: antipsychotics haloperidol^[14]^[9] perphenazine^[9]^[14] thioridazine^[14] zuclopenthixol^[14] risperidone^[14] chlorpromazine^[9] bicalutamide^[15] hyperforin (St. Johns Wort)^[16] antihistamines (H1-receptor antagonists) Promethazine^[17] chlorphenamine^[9] diphenhydramine^[9] hydroxyzine^[9] tripelennamine^[9] some SSRI antidepressants citalopram^[9] escitalopram^[9] clemastine^[9] (antihistamine and anticholinergic) celecoxib^[9] (NSAID) clomipramine^[9] (tricyclic antidepressant) cocaine^[9] (stimulant) doxorubicin^[9] (chemotherapeutic) metoclopramide^[9] (antiemetic, prokinetic) methadone^[9] (analgesic and anti-addictive) moclobemide^[9] (antidepressant) ranitidine^[9] (H2-receptor antagonist) doxepin^[9] (tricyclic antidepressant, anxiolytic) halofantrine^[9] (in malaria) levomepromazine^[9] (antipsychotic) mibefradil^[9] (calcium channel blocker) midodrine^[9] (α₁ agonist) ticlopidine^[9] (antiplatelet)	dexamethasone^[9] (glucocorticoid) rifampicin^[9] (bactericidal) strong: glutethimide (hypnotic sedative)

References

^

^ "Entrez Gene: CYP2D6 cytochrome P450, family 2, subfamily D, polypeptide 6". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1565.
^ Blake MJ, Gaedigk A, Pearce RE, Bomgaars LR, Christensen ML, Stowe C, James LP, Wilson JT, Kearns GL, Leeder JS (April 2007). "Ontogeny of dextromethorphan O- and N-demethylation in the first year of life". Clin. Pharmacol. Ther. 81 (4): 510–6. doi:10.1038/sj.clpt.6100101. PMID 17301735.
^ Lynch T, Price A (August 2007). "The effect of cytochrome P450 metabolism on drug response, interactions, and adverse effects". Am Fam Physician 76 (3): 391–6. PMID 17708140.
^ ^a ^b ^c Droll K, Bruce-Mensah K, Otton SV, Gaedigk A, Sellers EM, Tyndale RF (1998). "Comparison of three CYP2D6 probe substrates and genotype in Ghanaians, Chinese and Caucasians". Pharmacogenetics 8 (4): 325–33. doi:10.1097/00008571-199808000-00006. PMID 9731719.
^ Australian Medicines Handbook (AMH) 2004. ISBN 0-9578521-4-2
^ Gaedigk A, Bradford LD, Marcucci KA, Leeder JS (2002). "Unique CYP2D6 activity distribution and genotype-phenotype discordance in black Americans". Clin. Pharmacol. Ther. 72 (1): 76–89. doi:10.1067/mcp.2002.125783. PMID 12152006.
^ McLellan RA, Oscarson M, Seidegård J, Evans DA, Ingelman-Sundberg M (June 1997). "Frequent occurrence of CYP2D6 gene duplication in Saudi Arabians". Pharmacogenetics 7 (3): 187–91. doi:10.1097/00008571-199706000-00003. PMID 9241658.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab ^ac ^ad ^ae ^af ^ag ^ah ^ai ^aj ^ak ^al ^am ^an ^ao ^ap ^aq ^ar ^as ^at ^au ^av ^aw ^ax ^ay ^az ^ba ^bb ^bc ^bd ^be ^bf ^bg ^bh ^bi ^bj ^bk ^bl ^bm ^bn ^bo ^bp ^bq ^br ^bs ^bt ^bu ^bv ^bw ^bx ^by ^bz ^ca ^cb ^cc ^cd ^ce ^cf ^cg ^ch Flockhart DA (2007). "Drug Interactions: Cytochrome P₄₅₀ Drug Interaction Table". Indiana University School of Medicine. http://medicine.iupui.edu/flockhart/table.htm. Retrieved on July 2011
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab ^ac ^ad ^ae ^af FASS (drug formulary): Swedish environmental classification of pharmaceuticals Facts for prescribers (Fakta för förskrivare), retrieved July 2011
^ ^a ^b PHARMACOGENETICS AND PHARMACOGENOMICS. J. Steven Leeder PharmD, PhD Pediatric Clinics of North America - Volume 48, Issue 3 (June 2001). doi:10.1016/S0031-3955%2805%2970338-2.
^ Hoskins, J. M.; Carey, L. A.; McLeod, H. L. (2009). "CYP2D6 and tamoxifen: DNA matters in breast cancer". Nature Reviews Cancer 9 (8): 576. doi:10.1038/nrc2683. PMID 19629072. edit
^ Zhang W, Ramamoorthy Y, Tyndale RF, Sellers EM (June 2003). "Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro". Drug Metab. Dispos. 31 (6): 768–72. doi:10.1124/dmd.31.6.768. PMID 12756210.
^ ^a ^b ^c ^d ^e FASS, The Swedish official drug catalog > Kodein Recip Last reviewed 2008-04-08
^ Cockshott, I. D. (2004). "Bicalutamide: Clinical pharmacokinetics and metabolism". Clinical pharmacokinetics 43 (13): 855–878. PMID 15509184. edit
^ Foster BC, Sockovie ER, Vandenhoek S, Bellefeuille N, Drouin CE, Krantis A, Budzinski JW, Livesey J, and Arnason JT (2004). "In Vitro Activity of St. John's Wort Against Cytochrome P450 Isozymes and P-Glycoprotein ". Pharmaceutical Biology 42 (2): 159–169. doi:10.1080/13880200490512034.
^ He N, Zhang WQ, Shockley D, Edeki T (February 2002). "Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes". Eur. J. Clin. Pharmacol. 57 (12): 847–51. doi:10.1007/s00228-001-0399-0. PMID 11936702.

External links

Flockhart Lab Cyp2D6 Substrates Page at IUPUI
PharmGKB: Annotated PGx Gene Information for CYP2D6

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 薬理ゲノム学の概要 overview of pharmacogenomics
2. 選択的セロトニン再取り込み阻害剤：薬理学、投与方法、および副作用 selective serotonin reuptake inhibitors pharmacology administration and side effects
3. セロトニン - ノルエピネフリン再取り込み阻害剤（SNRIs）：薬理学、投与、および副作用 serotonin norepinephrine reuptake inhibitors snris pharmacology administration and side effects
4. 成人における抗癌剤の投与 dosing of anticancer agents in adults
5. オピオイド系薬剤を用いた癌疼痛のマネージメント：至適鎮痛作用 cancer pain management with opioids optimizing analgesia

English Journal

Evaluation of cytochrome P450-mediated drug-drug interactions based on the strategies recommended by regulatory authorities.

Kosugi Y, Hirabayashi H, Igari T, Fujioka Y, Hara Y, Okuda T, Moriwaki T.SourceDrug Metabolism and Pharmacokinetics Research Laboratories, Pharmaceutical Research Division, Takeda Pharmaceutical Company Limited , Yodogawa-ku, Osaka , Japan.
Xenobiotica; the fate of foreign compounds in biological systems.Xenobiotica.2012 Feb;42(2):127-38. Epub 2011 Nov 5.
Herein, we aimed to evaluate the recently proposed risk assessment strategies of a cytochrome P450 (CYP) mediated drug-drug interaction (DDI) according to the European Medicines Evaluation Agency (EMEA) draft guideline, and discuss the differences between this guideline and the Food and Drug Adminis
PMID 22117526

Label-free genotyping of cytochrome P450 2D6*10 using ligation-mediated strand displacement amplification with DNAzyme-based chemiluminescence detection.

Wang HQ, Wu Z, Zhang Y, Tang LJ, Yu RQ, Jiang JH.SourceState Key Laboratory of Chemo/Bio-Sensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, PR China; Research Center of Agricultural Quality Standards and Testing Techniques, Henan Academy of Agricultural Sciences, Zhengzhou 450002, PR China.
Analytica chimica acta.Anal Chim Acta.2012 Jan 13;710:111-7. Epub 2011 Nov 6.
Genotyping of cytochrome P450 monooxygenase 2D6*10 (CYP2D6*10) plays an important role in pharmacogenomics, especially in clinical drug therapy of Asian populations. This work reported a novel label-free technique for genotyping of CYP2D6*10 based on ligation-mediated strand displacement amplificati
PMID 22123119

Influence of CYP2D6 genotype on the disposition of the enantiomers of venlafaxine and its major metabolites in postmortem femoral blood.

Kingbäck M, Karlsson L, Zackrisson AL, Carlsson B, Josefsson M, Bengtsson F, Ahlner J, Kugelberg FC.SourceDivision of Drug Research, Clinical Pharmacology, Department of Medical and Health Sciences, Linköping University, Linköping, Sweden.
Forensic science international.Forensic Sci Int.2012 Jan 10;214(1-3):124-34. Epub 2011 Aug 12.
Venlafaxine (VEN) is an antidepressant drug mainly metabolized by the cytochrome P450 (CYP) enzyme CYP2D6 to the active metabolite O-desmethylvenlafaxine (ODV). VEN is also metabolized to N-desmetylvenlafaxine (NDV) via CYP3A4. ODV and NDV are further metabolized to N,O-didesmethylvenlafaxine (DDV).
PMID 21840145

Japanese Journal

Evolution of the CYP2D gene cluster in humans and four non-human primates

Yasukochi Yoshiki,Satta Yoko
Genes & genetic systems 86(2), 109-116, 2011-04
NAID 40018820924

Comparative Study of Culture Conditions for Maintaining CYP3A4 and ATP-Binding Cassette Transporters Activity in Primary Cultured Human Hepatocytes

Takeba Yuko,Matsumoto Naoki,Takenoshita-Nakaya Sachiko,Harimoto Yoshie,Kumai Toshio,Kinoshita Yuichi,Nakano Hiroshi,Ohtsubo Takehito,Kobayashi Shinichi
Journal of Pharmacological Sciences 115(4), 516-524, 2011
… Serum-free WEM and Lanford’s also maintained protein levels of CYP2C19, CYP2D6, and organic anion transporter polypeptide in the hepatocytes. …
NAID 130000663517

Related Pictures

Legend Pathway diagram How to cite this the cyp2d6 gene have a lot to do with this CYP2D6 Graph Description CYP2D6 structure.png El Camino Hospital - CYP2D6, CYP2C19, and CYP2D6 - Introduction Essay - Welcome to CYP2D6 CYP2 D6 Inhibitors http://www.fda.gov

★リンクテーブル★

リンク元	「シメチジン」
拡張検索	「CYP2D6タンパク質」「チトクロムP450酵素CYP2D6」「cytochrome P-450 CYP2D6」

「シメチジン」

Cytochrome P450, family 2, subfamily D, polypeptide 6
	; PDB rendering based on 2f9q.
Available structures
PDB	Ortholog search: PDBe, RCSB
List of PDB id codes
	2F9Q
Identifiers
Symbols	CYP2D6; CPD6; CYP2D; CYP2D7AP; CYP2D7BP; CYP2D7P2; CYP2D8P2; CYP2DL1; CYPIID6; P450-DB1; P450C2D; P450DB1
External IDs	OMIM: 124030 MGI: 1929474 HomoloGene: 68036 GeneCards: CYP2D6 Gene
EC number	1.14.14.1
Gene Ontology
Molecular function	• monooxygenase activity; • monooxygenase activity; • drug binding; • electron carrier activity; • oxidoreductase activity; • oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen; • heme binding; • heme binding; • metal ion binding; • aromatase activity;
Cellular component	• mitochondrion; • endoplasmic reticulum; • endoplasmic reticulum membrane; • microsome; • membrane;
Biological process	• xenobiotic metabolic process; • steroid metabolic process; • coumarin metabolic process; • alkaloid metabolic process; • alkaloid catabolic process; • monoterpenoid metabolic process; • drug metabolic process; • drug metabolic process; • isoquinoline alkaloid metabolic process; • 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 expression pattern
	More reference expression data
Orthologs
	This box: view; talk; edit;

　　[★]

英: cimetidine
商: アルキオーネ、イクロール、エスメラルダ、カイロック、シメチパール、シメチラン、シルカーゼット、ストマチジン、タカミジン、タガメット Tagamet、ダンスール、チーカプト、チスタメット、ファルジン
関: ヒスタミン受容体

消化性潰瘍治療薬

攻撃因子抑制剤

H₂ブロッカー = ヒスタミンH₂受容体選択的阻害薬

薬効薬理

シメチジン錠200mg「タナベ」／**シメチジン錠400mg「タナベ」／**シメチジン細粒20％「タナベ」

シメチジンは胃酸分泌抑制作用を示す．その作用機序は，胃粘膜細胞のヒスタミンのＨ2受容体に対する競合的拮抗作用による．ガストリン刺激，インスリン刺激及び食事刺激による胃酸分泌も抑制する．また，ペプシン分泌抑制作用も示す3）．

効能又は効果

シメチジン錠200mg「タナベ」／**シメチジン錠400mg「タナベ」／**シメチジン細粒20％「タナベ」

胃潰瘍，十二指腸潰瘍，吻合部潰瘍，Zollinger-Ellison症候群，逆流性食道炎，上部消化管出血（消化性潰瘍，急性ストレス潰瘍，出血性胃炎による）
下記疾患の胃粘膜病変（びらん，出血，発赤，浮腫）の改善

急性胃炎，慢性胃炎の急性増悪期

禁忌

シメチジン錠200mg「タナベ」／**シメチジン錠400mg「タナベ」／**シメチジン細粒20％「タナベ」

シメチジンに対し過敏症の既往歴のある患者

副作用

CYP2D6, CYP3A4阻害作用。これらはシメチジンとの相互作用が強い。多くの薬物代謝が影響を受ける。すなわち、副作用につながる
肝障害
抗アンドロゲン作用(女性化乳房、乳汁分泌)

相互作用

シメチジン（消化性潰瘍治療薬）→ビタミンB12の吸収低下？(根拠となる文献不明)
http://www2s.biglobe.ne.jp/~coop-dr/sougosayou.htm

添付文書

シメチジン錠200mg「タナベ」／**シメチジン錠400mg「タナベ」／**シメチジン細粒20％「タナベ」

http://www.info.pmda.go.jp/go/pack/2325001C1126_1_01/2325001C1126_1_01?view=body

「CYP2D6タンパク質」

　　[★]

英

(n

CYP2D6

関: チトクロムP450酵素CYP2D6

「チトクロムP450酵素CYP2D6」

　　[★]

英: cytochrome P-450 CYP2D6
関: CYP2D6タンパク質

「cytochrome P-450 CYP2D6」

　　[★]

チトクロムP450酵素CYP2D6

関: CYP2D6

[0] 

Cytochrome P450, family 2, subfamily D, polypeptide 6

PDB rendering based on 2f9q.

Available structures

PDB Ortholog search: PDBe, RCSB

List of PDB id codes

2F9Q

Identifiers

Symbols CYP2D6; CPD6; CYP2D; CYP2D7AP; CYP2D7BP; CYP2D7P2; CYP2D8P2; CYP2DL1; CYPIID6; P450-DB1; P450C2D; P450DB1

External IDs OMIM: 124030 MGI: 1929474 HomoloGene: 68036 GeneCards: CYP2D6 Gene

EC number 1.14.14.1

Gene Ontology

Molecular function • monooxygenase activity

• monooxygenase activity
• drug binding
• electron carrier activity
• oxidoreductase activity
• oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen
• heme binding
• heme binding
• metal ion binding

• aromatase activity

Cellular component • mitochondrion

• endoplasmic reticulum
• endoplasmic reticulum membrane
• microsome

• membrane

Biological process • xenobiotic metabolic process

• steroid metabolic process
• coumarin metabolic process
• alkaloid metabolic process
• alkaloid catabolic process
• monoterpenoid metabolic process
• drug metabolic process
• drug metabolic process
• isoquinoline alkaloid metabolic process
• 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 expression pattern

More reference expression data

Orthologs

Species Human Mouse

Entrez 1565 56448

Ensembl ENSG00000100197 ENSMUSG00000061740

UniProt P10635 Q9JKY7

RefSeq (mRNA) NM_000106.4 NM_001163472.1

RefSeq (protein) NP_000097.2 NP_001156944.1

Location (UCSC) Chr 22:
42.52 – 42.54 Mb Chr 15:
82.2 – 82.21 Mb

PubMed search [1] [2]

This box:

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talk

edit

[2] view

[3] talk

[4] t

[1] "Entrez Gene: CYP2D6 cytochrome P450, family 2, subfamily D, polypeptide 6". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=1565.

[pmid17301735-2] Blake MJ, Gaedigk A, Pearce RE, Bomgaars LR, Christensen ML, Stowe C, James LP, Wilson JT, Kearns GL, Leeder JS (April 2007). "Ontogeny of dextromethorphan O- and N-demethylation in the first year of life". Clin. Pharmacol. Ther. 81 (4): 510–6. doi:10.1038/sj.clpt.6100101. PMID 17301735.

[pmid17708140-3] Lynch T, Price A (August 2007). "The effect of cytochrome P450 metabolism on drug response, interactions, and adverse effects". Am Fam Physician 76 (3): 391–6. PMID 17708140.

[Droll_1998-4] Droll K, Bruce-Mensah K, Otton SV, Gaedigk A, Sellers EM, Tyndale RF (1998). "Comparison of three CYP2D6 probe substrates and genotype in Ghanaians, Chinese and Caucasians". Pharmacogenetics 8 (4): 325–33. doi:10.1097/00008571-199808000-00006. PMID 9731719.

[5] Australian Medicines Handbook (AMH) 2004. ISBN 0-9578521-4-2

[6] Gaedigk A, Bradford LD, Marcucci KA, Leeder JS (2002). "Unique CYP2D6 activity distribution and genotype-phenotype discordance in black Americans". Clin. Pharmacol. Ther. 72 (1): 76–89. doi:10.1067/mcp.2002.125783. PMID 12152006.

[pmid9241658-7] McLellan RA, Oscarson M, Seidegård J, Evans DA, Ingelman-Sundberg M (June 1997). "Frequent occurrence of CYP2D6 gene duplication in Saudi Arabians". Pharmacogenetics 7 (3): 187–91. doi:10.1097/00008571-199706000-00003. PMID 9241658.

[Flockhart-8] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab ^ac ^ad ^ae ^af ^ag ^ah ^ai ^aj ^ak ^al ^am ^an ^ao ^ap ^aq ^ar ^as ^at ^au ^av ^aw ^ax ^ay ^az ^ba ^bb ^bc ^bd ^be ^bf ^bg ^bh ^bi ^bj ^bk ^bl ^bm ^bn ^bo ^bp ^bq ^br ^bs ^bt ^bu ^bv ^bw ^bx ^by ^bz ^ca ^cb ^cc ^cd ^ce ^cf ^cg ^ch Flockhart DA (2007). "Drug Interactions: Cytochrome P₄₅₀ Drug Interaction Table". Indiana University School of Medicine. http://medicine.iupui.edu/flockhart/table.htm. Retrieved on July 2011

[FASS-9] ^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ ^j ^k ^l ^m ⁿ ^o ^p ^q ^r ^s ^t ^u ^v ^w ^x ^y ^z ^aa ^ab ^ac ^ad ^ae ^af FASS (drug formulary): Swedish environmental classification of pharmaceuticals Facts for prescribers (Fakta för förskrivare), retrieved July 2011

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[fass-codeine-13] FASS, The Swedish official drug catalog > Kodein Recip Last reviewed 2008-04-08

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[pmid11936702-16] He N, Zhang WQ, Shockley D, Edeki T (February 2002). "Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes". Eur. J. Clin. Pharmacol. 57 (12): 847–51. doi:10.1007/s00228-001-0399-0. PMID 11936702.

基質	反応
タモキシフェン	4-水酸化
フルボキサミン	O-脱メチル
ハロペリドール	N-脱アルキル
プロプラノロール	4-水酸化
コデイン	O-脱メチル

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CYP2D6

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