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cytochrome P450 2B6 (cytochrome P450 2B1, phenobarbital-inducible, CYP2B6)
Function:
1) NADPH-dependent electron transport pathway
2) oxidizes a variety of structurally unrelated compounds
- steroids, fatty acids, xenobiotics
3) phosphorylation decreases enzyme activity
4) inducers
- phenobarbital
5) substrates
- efavirenz
Compartment: membrane-bound, endoplasmic reticulum
Expression:
- expressed in liver, lung & heart right ventricle
- induced by phenobarbital
Polymorphism:
- polymorphisms can lead to accumulation of efavirenz & persistence after discontinuation [2]
Laboratory:
- CYP2B6 enzyme activity
- CYP2B6 gene mutation
General
cytochrome P450 2B (CYP2B)
phosphoprotein
Properties
SIZE: MW = 56 kD
entity length = 491 aa
COMPARTMENT: endoplasmic reticulum
MOTIF: Ser phosphorylation site {S128}
FOR-PHOSPHORYLATION-BY: protein kinase A
Iron [Fe]-binding site
SITE: 436-436
SUBSTRATE: efavirenz
INDUCERS: phenobarbital
Database Correlations
OMIM 123930
UniProt P20813
Entrez Gene 1555
ENZYME 1.14.14.1
References
- UniProt :accession P20813
- Ribaudo HJ et al,
Pharmacogenetics of plasma efavirenz exposure after treatment
discontinuation: An adult AIDS Clinical Trial Group Study.
Clin Infect Dis 2006; 42:401
PMID: 16392089
- Nolan D et al,
Efavirenz and CYP2B6 polymorphism: Implications for drug
toxicity and resistance.
Clin Infect Dis 2006; 42:408
PMID: 16392090
- Cytochrome P450 Allele Nomenclature committee, CYP2B6 alleles
http://www.cypalleles.ki.se/cyp2b6.htm