Cytochrome P450 2C9

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Cytochrome P450 2C9
Cytochrome P450 2C9
PDB  1R9O

Existing structural data : 1OG2 , 1OG5 , 1R9O , 4NZ2

Properties of human protein
Mass / length primary structure 55,628  Da / 490 AS
Cofactor Hamm
Identifier
Gene name CYP2C9
External IDs
Enzyme classification
EC, category 1.14.13 ,  oxidoreductase

CYP2C9 ( Cytochrome P450 2C9 ) belongs as isoenzyme to the subtypes of cytochrome P450 and is an enzyme which, when people through the CYP2C9 - gene is encoded.

Synonyms are: English CYPIIC9; Cytochrome P-450MP; Cytochrome P450 2C9; Cytochrome P450 MP-4; Cytochrome P450 MP-8; cytochrome P450 PB-1; cytochrome P450, family 2, subfamily C, polypeptide 9; P450 MP-4; S-mephenytoin 4-hydroxylase; S-mephenytoin 4-hydroxylase, human; warfarin-7-hydroxylase, human

The enzyme is produced in the endoplasmic reticulum and is the most widely expressed CYP2C enzyme in the liver.

It metabolizes u. a. Steroid hormones and fatty acids and plays an important role in the breakdown of various drugs such as the blood thinner S- warfarin , anti-inflammatory drugs such as ibuprofen , sulfonylureas , phenytoin , tolbutamide , losartan , terbinafine and tamoxifen , and is therefore of interest for assessing their effects.

Layout and function

CYP2C9 hydroxylates THC to 11-hydroxy-THC in the liver, among other things . It is - among other P-450 isoenzymes - important for the drug treatment of depression , as it is inhibited by various antidepressants such as fluoxetine , fluvoxamine , sertraline and paroxetine . It is also associated with a reduced metabolism of coumarin , an anticoagulant .

The enzyme can be inhibited by fluconazole and miconazole .

literature

  • A. Seeringer, J. Kirchheiner: CYP2D6, CYP2C9, and CYP2C19-based drug dose adjustments. When do they make sense? In: The internist . Vol. 49, No. 7, July 2008, pp. 877-883, doi : 10.1007 / s00108-008-2125-9 , PMID 18551264 (review).
  • M. Romkes, MB Faletto, JA Blaisdell, JL Raucy, JA Goldstein: Cloning and expression of complementary DNAs for multiple members of the human cytochrome P450IIC subfamily. In: Biochemistry . Vol. 30, No. 13, April 1991, pp. 3247-3255, PMID 2009263 .
  • K. Inoue, J. Inazawa, Y. Suzuki, T. Shimada, H. Yamazaki, FP Guengerich, T. Abe: Fluorescence in situ hybridization analysis of chromosomal localization of three human cytochrome P450 2C genes (CYP2C8, 2C9, and 2C10) at 10q24.1. In: The Japanese journal of human genetics. Vol. 39, No. 3, September 1994, pp. 337-343, doi : 10.1007 / BF01874052 , PMID 7841444 .

Individual evidence

  1. ↑ UniProt P11712 .
  2. ↑ a b c Entry on CYP2C9 in the Flexikon , a Wiki of the DocCheck company
  3. ↑ a b CYTOCHROME P450, SUBFAMILY IIC, POLYPEPTIDE 9; CYP2C9.  In: Online Mendelian Inheritance in Man . (English)
  4. ↑ a b Genetics Home Reference
  5. ↑ Thomas Efferth: Molecular pharmacology and toxicology: biological bases of drugs and poisons . Springer, Berlin, Heidelberg, New York 2006, ISBN 3-540-21223-X , pp. 22 .
  6. ↑ Rudolf Hänsel, Ernst Steinegger (Ed.): Pharmakognosie - Phytopharmazie . 9., revised. and updated edition. Springer, Heidelberg 2010, ISBN 978-3-642-00962-4 , pp. 1158 .
  7. ↑ Hasso Scholz, Gustav Kuschinsky, Rainer Böger (ed.): Pocket book of drug treatment: applied pharmacology . 13., revised. and updated edition. Springer, Berlin, Heidelberg, New York 2005, ISBN 3-540-20821-6 , pp. 247 .
  8. ↑ Axel M. Gressner, Torsten Arndt (Ed.): Lexicon of the Medical Laboratory Diagnostics . 2nd, revised and expanded edition. Springer, Berlin, Heidelberg 2013, ISBN 978-3-642-12921-6 , entry on coumarin sensitivity , urn : nbn: de: 1111-20130111292 .