CYP2C8

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Cytochrome P450, family 2, subfamily C, polypeptide 8
Protein CYP2C8 PDB 1pq2.png
PDB rendering based on 1pq2.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols CYP2C8 ; CPC8; CYPIIC8; MP-12/MP-20
External IDs OMIM601129 MGI1917138 HomoloGene117948 ChEMBL: 3721 GeneCards: CYP2C8 Gene
EC number 1.14.14.1
RNA expression pattern
PBB GE CYP2C8 208147 s at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 1558 13095
Ensembl ENSG00000138115 ENSMUSG00000003053
UniProt P10632 Q64458
RefSeq (mRNA) NM_000770 NM_007815
RefSeq (protein) NP_000761 NP_031841
Location (UCSC) Chr 10:
96.8 – 96.83 Mb
Chr 19:
39.27 – 39.33 Mb
PubMed search [1] [2]

Cytochrome P4502C8 (abbreviated CYP2C8), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body.

CYP2C8 Ligands[edit]

Following is a table of selected substrates, inducers and inhibitors of 2C8.

Inhibitors of CYP2C8 can be classified by their potency, such as:

  • Strong inhibitor being one that causes at least a five-fold increase in the plasma AUC values, or more than 80% decrease in clearance.[1]
  • Moderate inhibitor being one that causes at least a two-fold increase in the plasma AUC values, or 50-80% decrease in clearance.[1]
  • Weak inhibitor being one that causes at least a 1.25-fold but less than two-fold increase in the plasma AUC values, or 20-50% decrease in clearance.[1]
Selected inducers, inhibitors and substrates of CYP2C8
Substrates Inhibitors Inducers

Strong:

Moderate

Unspecified potency

Where classes of agents are listed, there may be exceptions within the class.

See also[edit]

References[edit]

  1. ^ a b c d e f g h i j k l m n o Flockhart DA (2007). "Drug Interactions: Cytochrome P450 Drug Interaction Table". Indiana University School of Medicine.  Retrieved on July 2011
  2. ^ Chapter 26 in: Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). Rang & Dale's pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-06911-5. 

Further reading[edit]

  • Goldstein JA, de Morais SM (1995). "Biochemistry and molecular biology of the human CYP2C subfamily.". Pharmacogenetics 4 (6): 285–99. doi:10.1097/00008571-199412000-00001. PMID 7704034. 
  • Smith G, Stubbins MJ, Harries LW, Wolf CR (1999). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily.". Xenobiotica 28 (12): 1129–65. doi:10.1080/004982598238868. PMID 9890157. 
  • García-Martín E, Martínez C, Ladero JM, Agúndez JA (2007). "Interethnic and intraethnic variability of CYP2C8 and CYP2C9 polymorphisms in healthy individuals.". Molecular diagnosis & therapy 10 (1): 29–40. doi:10.1007/BF03256440. PMID 16646575. 
  • Ged C, Beaune P (1991). "Isolation of the human cytochrome P-450 IIC8 gene: multiple glucocorticoid responsive elements in the 5' region.". Biochim. Biophys. Acta 1088 (3): 433–5. doi:10.1016/0167-4781(91)90138-c. PMID 1707679. 
  • Romkes M, Faletto MB, Blaisdell JA, et al. (1991). "Cloning and expression of complementary DNAs for multiple members of the human cytochrome P450IIC subfamily.". Biochemistry 30 (13): 3247–55. doi:10.1021/bi00227a012. PMID 2009263. 
  • Kolyada AY (1990). "Sequence of a human liver cytochrome P-450 cDNA clone". Nucleic Acids Res. 18 (18): 5550. doi:10.1093/nar/18.18.5550. PMC 332242. PMID 2216732. 
  • Shephard EA, Phillips IR, Santisteban I, et al. (1989). "Cloning, expression and chromosomal localization of a member of the human cytochrome P450IIC gene sub-family". Ann. Hum. Genet. 53 (Pt 1): 23–31. doi:10.1111/j.1469-1809.1989.tb01119.x. PMID 2729895. 
  • Ged C, Umbenhauer DR, Bellew TM, et al. (1989). "Characterization of cDNAs, mRNAs, and proteins related to human liver microsomal cytochrome P-450 (S)-mephenytoin 4'-hydroxylase". Biochemistry 27 (18): 6929–40. doi:10.1021/bi00418a039. PMID 3196692. 
  • Okino ST, Quattrochi LC, Pendurthi UR, et al. (1987). "Characterization of multiple human cytochrome P-450 1 cDNAs. The chromosomal localization of the gene and evidence for alternate RNA splicing". J. Biol. Chem. 262 (33): 16072–9. PMID 3500169. 
  • Kimura S, Pastewka J, Gelboin HV, Gonzalez FJ (1988). "cDNA and amino acid sequences of two members of the human P450IIC gene subfamily". Nucleic Acids Res. 15 (23): 10053–4. doi:10.1093/nar/15.23.10053. PMC 306558. PMID 3697070. 
  • Zeldin DC, DuBois RN, Falck JR, Capdevila JH (1995). "Molecular cloning, expression and characterization of an endogenous human cytochrome P450 arachidonic acid epoxygenase isoform". Arch. Biochem. Biophys. 322 (1): 76–86. doi:10.1006/abbi.1995.1438. PMID 7574697. 
  • Inoue K, Inazawa J, Suzuki Y, et al. (1995). "Fluorescence in situ hybridization analysis of chromosomal localization of three human cytochrome P450 2C genes (CYP2C8, 2C9, and 2C10) at 10q24.1". Jpn. J. Hum. Genet. 39 (3): 337–43. doi:10.1007/BF01874052. PMID 7841444. 
  • Gray IC, Nobile C, Muresu R, et al. (1996). "A 2.4-megabase physical map spanning the CYP2C gene cluster on chromosome 10q24". Genomics 28 (2): 328–32. doi:10.1006/geno.1995.1149. PMID 8530044. 
  • Wormhoudt LW, Ploemen JH, de Waziers I, et al. (1996). "Inter-individual variability in the oxidation of 1,2-dibromoethane: use of heterologously expressed human cytochrome P450 and human liver microsomes". Chem. Biol. Interact. 101 (3): 175–92. doi:10.1016/0009-2797(96)03723-4. PMID 8870687. 
  • McFayden MC, Melvin WT, Murray GI (1998). "Regional distribution of individual forms of cytochrome P450 mRNA in normal adult human brain". Biochem. Pharmacol. 55 (6): 825–30. doi:10.1016/S0006-2952(97)00516-9. PMID 9586955. 
  • Macé K, Bowman ED, Vautravers P, et al. (1998). "Characterisation of xenobiotic-metabolising enzyme expression in human bronchial mucosa and peripheral lung tissues". Eur. J. Cancer 34 (6): 914–20. doi:10.1016/S0959-8049(98)00034-3. PMID 9797707. 
  • Klose TS, Blaisdell JA, Goldstein JA (1999). "Gene structure of CYP2C8 and extrahepatic distribution of the human CYP2Cs". J. Biochem. Mol. Toxicol. 13 (6): 289–95. doi:10.1002/(SICI)1099-0461(1999)13:6<289::AID-JBT1>3.0.CO;2-N. PMID 10487415. 
  • Finta C, Zaphiropoulos PG (2000). "The human CYP2C locus: a prototype for intergenic and exon repetition splicing events". Genomics 63 (3): 433–8. doi:10.1006/geno.1999.6063. PMID 10704292.