Key Summary of CYP3A4:

Molecular Structure

• Most abundant enzyme in liver's P450 system
• Spacious active site capable of expanding from 950 to 1,650 cubic angstroms
• Dynamic binding region allows processing of various molecular sizes

Regulatory Mechanisms

• Controlled by nuclear receptors like PXR and CAR
• Influenced by epigenetic changes including DNA methylation
• Transcription regulated by long noncoding RNAs and microRNAs

Genetic Variations

• Over 30 nucleotide polymorphisms impact enzyme function
• Specific variants like CYP3A422 and CYP3A41B affect drug metabolism
• Critical for personalized medicine and treatment optimization

Drug Interactions

• Metabolizes approximately 50% of market drugs
• Potential for competitive inhibition and enzyme induction
• Interactions can significantly alter drug effectiveness and blood levels

Emerging Research

• Potential therapeutic targeting approach
• Exploring impacts on gut-liver connection
• Investigating nanotechnology for drug delivery bypassing enzyme processing