CYP3A4 (cytochrome P450 family 3 subfamily A member 4)
- symbol:
- CYP3A4
- locus group:
- protein-coding gene
- location:
- 7q22.1
- gene_family:
- Cytochrome P450s
- alias symbol:
- None
- alias name:
- None
- entrez id:
- 1576
- ensembl gene id:
- ENSG00000160868
- ucsc gene id:
- uc064fwx.1
- refseq accession:
- NM_001202855
- hgnc_id:
- HGNC:2637
- approved reserved:
- 1990-02-24
CYP3A4是细胞色素P450超家族中CYP3A亚家族的重要成员，位于人类7号染色体上。作为肝脏和肠道中含量最丰富的代谢酶，CYP3A4主要负责代谢约50%的临床常用药物，包括他汀类降脂药、抗肿瘤药和抗生素等。它通过氧化反应将脂溶性药物转化为水溶性代谢物以利于排泄。CYP3A4具有广泛的底物特异性，其活性受遗传多态性、药物诱导或抑制等因素显著影响。该基因的突变可能导致酶活性改变，例如CYP3A4*1B突变与前列腺癌风险相关，而*22等位基因则导致酶活性降低。CYP3A4过表达会加速药物代谢，降低疗效；表达不足则可能引发药物蓄积中毒。它与CYP3A5、CYP3A7等组成CYP3A基因家族，这些同工酶具有相似的底物特异性但组织分布和发育表达模式不同。CYP3A4还参与类固醇激素代谢，其表达受孕烷X受体（PXR）和组成型雄烷受体（CAR）调控。临床上，CYP3A4介导的药物相互作用非常常见，如葡萄柚汁中的呋喃香豆素可不可逆地抑制其活性。该酶的个体差异可达40倍，是实施个体化用药时需重点考虑的遗传因素之一。
This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases that catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by glucocorticoids and some pharmacological agents. This enzyme is involved in the metabolism of approximately half the drugs in use today, including acetaminophen, codeine, cyclosporin A, diazepam and erythromycin. The enzyme also metabolizes some steroids and carcinogens. This gene is part of a cluster of cytochrome P450 genes on chromosome 7q21.1. Previously another CYP3A gene, CYP3A3, was thought to exist; however, it is now thought that this sequence represents a transcript variant of CYP3A4. Alternatively spliced transcript variants encoding different isoforms have been identified. [provided by RefSeq, Feb 2011]
该基??因编码的酶的细胞色素P450超家族的成员。细胞色素P450蛋白是催化涉及药物代谢和胆固醇，类固醇和其他脂类的合成许多反应单加氧酶。此蛋白质定位于内质网和它的表达是由糖皮质激素和某些药理学药剂诱导的。这种酶是参与的大约一半在目前使用的药物，包括对乙酰氨基酚，可待因，环孢菌素A，地西泮和红霉素的代谢。酶还代谢一些类固醇和致癌物质。这种基因是细胞色素P450基因在染色体7q21.1群集的一部分。此前另一CYP3A基因??CYP3A3，被认为存在;然而，它现在认为这个序列表示CYP3A4的转录变异体。编码不同同种型的可变剪接转录物变体也已确定。 [由RefSeq的，2011年2月提供]
基因本体信息
CYP3A4基因（以及对应的蛋白质）的细胞分布位置：
- 质膜
- 细胞质
- 细胞外
- 高尔基体
- 囊泡
- 细胞骨架
- 内质网
- 细胞核
- 内体
- 溶酶体
- 线粒体
CYP3A4基因的本体（GO）信息：
| 名称 |
|---|
| 140 Steroid hormone biosynthesis [PATH:hsa00140] |
| 591 Linoleic acid metabolism [PATH:hsa00591] |
| 830 Retinol metabolism [PATH:hsa00830] |
| 980 Metabolism of xenobiotics by cytochrome P450 [PATH:hsa00980] |
| 982 Drug metabolism - cytochrome P450 [PATH:hsa00982] |
| 983 Drug metabolism - other enzymes [PATH:hsa00983] |
| 4976 Bile secretion [PATH:hsa04976] |
| 5204 Chemical carcinogenesis [PATH:hsa05204] |
| 名称 |
|---|
| Aflatoxin activation and detoxification |
| Biological oxidations |
| Cytochrome P450 - arranged by substrate type |
| Metabolism |
| Phase 1 - Functionalization of compounds |
| Xenobiotics |
| 疾病名称 | 关系值 | NofPmids | NofSnps | 来源 |
| Mammary Neoplasms | 0.133635564 | 10 | 0 | BeFree_CTD_human_GAD_LHGDN |
| Prostatic Neoplasms | 0.122995792 | 3 | 0 | BeFree_CTD_human_LHGDN |
| Osteosarcoma | 0.12272435 | 1 | 0 | CTD_human_LHGDN |
| Hepatitis C | 0.120542884 | 3 | 0 | BeFree_CTD_human |
| Torsades de Pointes | 0.12 | 1 | 0 | CTD_human |
| Diabetes Mellitus, Non-Insulin-Dependent | 0.093006804 | 7 | 0 | BeFree_CTD_rat_GAD_LHGDN |
| Kidney Failure, Chronic | 0.080542884 | 3 | 0 | BeFree_RGD |
| Inflammation | 0.08 | 1 | 0 | CTD_rat |
| Anxiety Disorders | 0.08 | 1 | 0 | RGD |
| Malignant neoplasm of prostate | 0.050749832 | 39 | 0 | BeFree_GAD |
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