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cytochrome P450 2C8; cytochrome P450 2C2, cytochrome P450 form 1; cytochrome P450 MP-12/MP-20; S-mephenytoin-4-hydroxylase (CYP2C8)

Function: 1) NADPH-dependent electron transport pathway 2) oxidizes a variety of structurally unrelated compounds a) steroids b) fatty acids - in the epoxidation of arachidonic acid, generates only 14,15- & 11,12-cis-epoxyeicosatrienoic acids c) xenobiotics 3) inducers - carbamazepine - nilotinib - phenobarbital - rifabutin - rifampicin - rifampin 4) inhibitors - atazanavir - anastrozole - gemfibrozil - lapatinib - montelukast - nicardipine - nilotinib - pazopanib - quercetin - sorafenib - sulfinpyrazone - trimethoprim - vilazodone 5) substrates - amiodarone - benzphetamine - carbamazepine - docetaxel - fluvastatin - isotretinoin - lapatinib - methadone - paclitaxel - phenytoin - pioglitazone - repaglinide - retinoic acid - retinol - rosiglitazone - tolbutamide - tretinoin - verapamil - warfarin - zopiclone Compartment: membrane-bound, endoplasmic reticulum Alternative splicing: - occurs, but the shorter forms are believed to be non-functional Expression: induced by phenobarbital (see inducers) Laboratory: - CYP2C8 gene mutation

General

cytochrome P450 2C (CYP2C)

Properties

SIZE: MW = 56 kD entity length = 490 aa COMPARTMENT: endoplasmic reticulum MOTIF: Iron [Fe]-binding site SITE: 435-435 SUBSTRATE: amiodarone benzphetamine carbamazepine docetaxel fluvastatin 13-cis retinoic acid lapatinib methadone paclitaxel phenytoin pioglitazone repaglinide retinoic acid retinol rosiglitazone tolbutamide all-trans retinoic acid verapamil warfarin zopiclone INDUCERS: carbamazepine nilotinib phenobarbital rifabutin rifampin rifampin INHIBITORS: atazanavir anastrozole gemfibrozil lapatinib montelukast nicardipine nilotinib pazopanib quercetin sorafenib sulfinpyrazone trimethoprim vilazodone

Database Correlations

OMIM 601129 UniProt P10632 Pfam PF00067 Entrez Gene 1558 Kegg hsa:1558 ENZYME 1.14.14.1

References

  1. OMIM :accession 124020
  2. Prescriber's Letter Cytochrome P450 drug interactions Detail-Document#: 150400 Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  3. Cytochrome P450 Allele Nomenclature committee, CYP2C8 alleles http://www.cypalleles.ki.se/cyp2c8.htm
  4. UniProt :accession P10632
  5. Prescriber's Letter 18(3): 2011 CHART: Cytochrome P450 Drug Interactions Detail-Document#: 270307 (subscription needed) http://www.prescribersletter.com