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Cytochrome P450 Superfamily
CYP450 proteins are primarily membrane-bound proteins that are involved in the metabolism of various molecules
- Introduction
- Function
- Role in Drug Metabolism
- Expression
- Specific CYP450 Molecules
- Role in Disease
- Structure
- Gene and Processing
Introduction
- Over 50 human CYP450 genes have been discovered
Function
- CYP450 proteins can metabolize various substrates. Drug metabolism is a critical function of CYP450 molecules
Role in Drug Metabolism
- families 1-3 involved with drug metabolism
- CYP3A4 is most relevant - 50-70% of drugs
- abundant in SI and liver
- very broad substrate specificity
- inhibitors: antifungals (ie ketoconazole), antibiotics (ie erythromycin), grapefruit juice
- most common cause of ADRs
- inducers: anticonvulsants (carbamazepine, phenobarbital), steriods (pregnenolone, dexamethasone), HIV protease inhibitors (saquinavir) antibiotics (rifampicin), St John's Wort
Expression
- CYP450 proteins are found in the largest amount in the liver, where they encounter molecules coming from the GI system
- other sites include the GI mucosa
Specific CYP450 Molecules
Role in Disease
- if any
Structure
- template
Gene and Processing
- PubMed ref: here
- other info