From Wikipedia, the free encyclopedia
Jump to: navigation, search
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
Symbols CYP2C8 ; CPC8; CYPIIC8; MP-12/MP-20
External IDs OMIM601129 MGI1917138 HomoloGene117948 ChEMBL: 3721 GeneCards: CYP2C8 Gene
EC number
RNA expression pattern
PBB GE CYP2C8 208147 s at tn.png
More reference expression data
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:
95.04 – 95.07 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



Unspecified potency

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

See also[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.