Inhibitors of CYP2C8 can be classified by theirpotency, such as:
Strong inhibitor being one that causes at least a five-fold increase in the plasmaAUC values, or more than 80% decrease inclearance.[6]
Moderate inhibitor being one that causes at least a two-fold increase in the plasma AUC values, or 50-80% decrease in clearance.[6]
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.[6]
Selected inducers, inhibitors and substrates of CYP2C8
Along with CYP2C8,CYP2C9,CYP2C19,CYP2J2, and possiblyCYP2S1 are the main producers of EETs and, very likely, EEQs, EDPs, and the epoxides of linoleic acid.[12][13]
^Chapter 26 in:Rod Flower, Humphrey P. Rang, Maureen M. Dale, Ritter, James M. (2007).Rang & Dale's pharmacology. Edinburgh: Churchill Livingstone.ISBN978-0-443-06911-6.
^Fleming I (October 2014). "The pharmacology of the cytochrome P450 epoxygenase/soluble epoxide hydrolase axis in the vasculature and cardiovascular disease".Pharmacological Reviews.66 (4):1106–40.doi:10.1124/pr.113.007781.PMID25244930.S2CID39465144.
^Shahabi P, Siest G, Meyer UA, Visvikis-Siest S (November 2014). "Human cytochrome P450 epoxygenases: variability in expression and role in inflammation-related disorders".Pharmacology & Therapeutics.144 (2):134–61.doi:10.1016/j.pharmthera.2014.05.011.PMID24882266.
Goldstein JA, de Morais SM (Dec 1994). "Biochemistry and molecular biology of the human CYP2C subfamily".Pharmacogenetics.4 (6):285–99.doi:10.1097/00008571-199412000-00001.PMID7704034.
Smith G, Stubbins MJ, Harries LW, Wolf CR (Dec 1998). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily".Xenobiotica.28 (12):1129–65.doi:10.1080/004982598238868.PMID9890157.
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.PMID16646575.S2CID25261882.
Ged C, Beaune P (Mar 1991). "Isolation of the human cytochrome P-450 IIC8 gene: multiple glucocorticoid responsive elements in the 5' region".Biochimica et Biophysica Acta.1088 (3):433–5.doi:10.1016/0167-4781(91)90138-c.PMID1707679.
Romkes M, Faletto MB, Blaisdell JA, Raucy JL, Goldstein JA (Apr 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.PMID2009263.
Shephard EA, Phillips IR, Santisteban I, Palmer CN, Povey S (Jan 1989). "Cloning, expression and chromosomal localization of a member of the human cytochrome P450IIC gene sub-family".Annals of Human Genetics.53 (Pt 1):23–31.doi:10.1111/j.1469-1809.1989.tb01119.x.PMID2729895.S2CID32620206.
Ged C, Umbenhauer DR, Bellew TM, Bork RW, Srivastava PK, Shinriki N, Lloyd RS, Guengerich FP (Sep 1988). "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.PMID3196692.
Zeldin DC, DuBois RN,Falck JR, Capdevila JH (Sep 1995). "Molecular cloning, expression and characterization of an endogenous human cytochrome P450 arachidonic acid epoxygenase isoform".Archives of Biochemistry and Biophysics.322 (1):76–86.doi:10.1006/abbi.1995.1438.PMID7574697.
Gray IC, Nobile C, Muresu R, Ford S, Spurr NK (Jul 1995). "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.PMID8530044.
Wormhoudt LW, Ploemen JH, de Waziers I, Commandeur JN, Beaune PH, van Bladeren PJ, Vermeulen NP (Sep 1996). "Inter-individual variability in the oxidation of 1,2-dibromoethane: use of heterologously expressed human cytochrome P450 and human liver microsomes".Chemico-Biological Interactions.101 (3):175–92.Bibcode:1996CBI...101..175W.doi:10.1016/0009-2797(96)03723-4.PMID8870687.
McFayden MC, Melvin WT, Murray GI (Mar 1998). "Regional distribution of individual forms of cytochrome P450 mRNA in normal adult human brain".Biochemical Pharmacology.55 (6):825–30.doi:10.1016/S0006-2952(97)00516-9.PMID9586955.
Macé K, Bowman ED, Vautravers P, Shields PG, Harris CC, Pfeifer AM (May 1998). "Characterisation of xenobiotic-metabolising enzyme expression in human bronchial mucosa and peripheral lung tissues".European Journal of Cancer.34 (6):914–20.doi:10.1016/S0959-8049(98)00034-3.PMID9797707.
Finta C, Zaphiropoulos PG (Feb 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.PMID10704292.