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Cytochrome P450 3A4 (abbreviated CYP3A4) ( EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by CYP3A4 gene. It oxidizes small foreign organic molecules ( xenobiotics ), such as toxins or drugs, so that they can be removed from the body.
- CYP3A4, CP33, CP34, CYP3A, CYP3A3, CYPIIIA3, CYPIIIA4, HLP, NF-25, P450C3, P450PCN1, cytochrome P450 family 3 subfamily A member 4, VDDR3
CYP3A4, CYP3A5, CYP3A7, and CYP3A43. The region also contains four pseudogenes: CYP3A51P, CYP3A52P, CYP3A54P, and CYP3A137P. as well as several extra exons which may or may not be included in transcripts produced from this region.
- CYP3A, cytochrome P450, family 3, subfamily A, CYP3
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- Nomenclature
- Classification
- Mechanism
- P450s in Humans
- P450s in Other Species
- InterPro Subfamilies
- See Also
- External Links
Genes encoding P450 enzymes, and the enzymes themselves, are designated with the root symbol CYP for the superfamily, followed by a number indicating the gene family, a capital letter indicating the subfamily, and another numeral for the individual gene. The convention is to italicise the name when referring to the gene. For example, CYP2E1 is the ...
Based on the nature of the electron transfer proteins, P450s can be classified into several groups: Microsomal P450 systems 1. in which electrons are transferred from NADPH via cytochrome P450 reductase (variously CPR, POR, or CYPOR). Cytochrome b5 (cyb5) can also contribute reducing power to this system after being reduced by cytochrome b5 reducta...
Structure
The active site of cytochrome P450 contains a heme-iron center. The iron is tethered to the protein via a cysteine thiolate ligand. This cysteine and several flanking residues are highly conserved in known P450s, and have the formal PROSITE signature consensus pattern [FW] - [SGNH] - x - [GD] - {F} - [RKHPT] - {P} - C - [LIVMFAP] - [GAD].Because of the vast variety of reactions catalyzed by P450s, the activities and properties of the many P450s differ in many aspects. In general, the P450 cat...
Catalytic cycle
1. Substrate binds in proximity to the heme group, on the side opposite to the axial thiolate. Substrate binding induces a change in the conformation of the active site, often displacing a water molecule from the distal axial coordination position of the heme iron,and changing the state of the heme iron from low-spin to high-spin. 2. Substrate binding induces electron transfer from NAD(P)H via cytochrome P450 reductase or another associated reductase. 3. Molecular oxygen binds to the resultin...
Spectroscopy
Binding of substrate is reflected in the spectral properties of the enzyme, with an increase in absorbance at 390 nm and a decrease at 420 nm. This can be measured by difference spectroscopies and is referred to as the "type I" difference spectrum (see inset graph in figure). Some substrates cause an opposite change in spectral properties, a "reverse type I" spectrum, by processes that are as yet unclear. Inhibitors and certain substrates that bind directly to the heme iron give rise to the t...
Human P450s are primarily membrane-associated proteins located either in the inner membrane of mitochondria or in the endoplasmic reticulum of cells. P450s metabolize thousands of endogenous and exogenous chemicals. Some P450s metabolize only one (or a very few) substrates, such as CYP19 (aromatase), while others may metabolize multiple substrates....
Animals
Other animals often have more P450 genes than humans do. Reported numbers range from 35 genes in the sponge Amphimedon queenslandica to 235 genes in the cephalochordate Branchiostoma floridae. Mice have genes for 101 P450s, and sea urchins have even more (perhaps as many as 120 genes).Most CYP enzymes are presumed to have monooxygenase activity, as is the case for most mammalian CYPs that have been investigated (except for, e.g., CYP19 and CYP5). Gene and genome sequencing is far outpacing bi...
Microbial
Microbial cytochromes P450 are often soluble enzymes and are involved in diverse metabolic processes. In bacteria the distribution of P450s is very variable with many bacteria having no identified P450s (e.g. E.coli). Some bacteria, predominantly actinomycetes, have numerous P450s (e.g.,). Those so far identified are generally involved in either biotransformation of xenobiotic compounds (e.g. CYP105A1 from Streptomyces griseolus metabolizes sulfonylurea herbicides to less toxic derivatives,)...
Fungi
The commonly used azole class of antifungal drugs works by inhibition of the fungal cytochrome P450 14α-demethylase.[better source needed]
InterProsubfamilies: 1. Cytochrome P450, B-class InterPro: IPR002397 2. Cytochrome P450, mitochondrial InterPro: IPR002399 3. Cytochrome P450, E-class, group I InterPro: IPR002401 4. Cytochrome P450, E-class, group II InterPro: IPR002402 5. Cytochrome P450, E-class, group IV InterPro: IPR002403 6. Aromatase Clozapine, imipramine, paracetamol, phena...
Degtyarenko K (2009-01-09). "Directory of P450-containing Systems". International Centre for Genetic Engineering and Biotechnology. Archived from the original on 2016-07-16. Retrieved 2009-02-10.Flockhart DA (2008-09-04). "Human Cytochrome P450 (CYP) Allele Nomenclature Committee". Karolinska Institutet. Retrieved 2009-02-10.Preissner S (2010). "Cytochrome P450 database". Nucleic Acids Research. Archived from the original on 2011-11-03. Retrieved 2011-08-02.Sigaroudi A, Vollbrecht H (2019). "pharmacokinetic interaction table". Sigaroudi & Vollbrecht.CYP3A4 and CYP3A5 together account for approximately 30% of hepatic cytochrome P450, and approximately half of medications that are oxidatively metabolized by P450 are CYP3A substrates. Both CYP3A4 and CYP3A5 are expressed in liver and intestine, with CYP3A5 being the predominant form expressed in extrahepatic tissues.
PopulationCyp3a5*1Cyp3a5*312%88%35%65%63%37%19%81%- CYP3A5, CP35, CYPIIIA5, P450PCN3, PCN3, cytochrome P450 family 3 subfamily A member 5
CYP3A43. Cytochrome P450 3A43 is a protein that in humans is encoded by the CYP3A43 gene. [3] [4] [5] This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
- CYP3A43, cytochrome P450 family 3 subfamily A member 43
CYP3A7 is an enzyme belonging to the cytochrome P450 family. It is 503 amino acids in size and shares 87% of its sequence with CYP3A4. It carries out a similar role in fetuses that CYP3A4 serves in adults. [5] The gene location is 7q22.1.
CYP3A4 Amiodarone Aprepitant Bergamottin Buprenorphine Cafestol Chloramphenicol Cimetidine Ciprofloxacin Clarithromycin Cobicistat Delavirdine Diltiazem Dithiocarbamate Domperidone Erythromycin Esomeprazole Fluconazole Fluvoxamine Gestodene
