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review · Biomedicines

Decoding the Role of CYP450 Enzymes in Metabolism and Disease: A Comprehensive Review

202496 citationsOpen accessModern Sciences and Arts University

In plain language

Cytochrome P450 enzymes encompass fifty-seven functional genes across eighteen families, with the CYP1, CYP2, and CYP3 families being particularly prominent. These enzymes are central to Phase I drug metabolism and process essential endogenous compounds, including lipids, proteins, and hormones. Disruption of their normal activity is linked to various endocrine disorders, as well as alterations in fatty acid processing, cholesterol production, and bile acid biosynthesis. Consequently, CYP450 enzymes offer therapeutic relevance for conditions such as hypercholesterolemia and neurodegenerative disorders. Furthermore, these enzymes influence cancer development and affect the success of chemotherapy treatments. Measuring CYP450 expression and activity provides critical diagnostic insight into liver health, helping clinicians differentiate between liver conditions and adjust medical interventions. Ultimately, evaluating CYP450 activity and genetic variations offers a pathway to tailor personalised therapies and improve drug responses across diverse populations.

Key takeaways

  • The human genome contains 57 functional CYP450 genes across 18 families, with CYP1, CYP2, and CYP3 playing prominent roles in metabolism.
  • Beyond drug processing, CYP450 enzymes regulate endogenous lipids, proteins, and hormones, influencing conditions such as hypercholesterolemia and neurodegenerative diseases.
  • CYP450 enzymes are implicated in cancer onset and significantly affect chemotherapy outcomes.
  • Evaluating CYP450 expression, activity, and genetic polymorphisms provides diagnostic tools for liver disease and informs personalised therapeutic strategies.

Why it matters

Variability in CYP450 enzyme function directly influences how individuals process medications and maintain metabolic health. Because these enzymes are tied to critical conditions, including liver disease, cancer, and endocrine disorders, understanding their biological roles helps clinicians anticipate treatment outcomes. This knowledge is essential for tailoring medical therapies to individual genetic profiles, thereby improving drug safety and therapeutic effectiveness across diverse patient groups.

Commercialisation angle

The findings point towards applications in diagnostic liver profiling, therapeutic targeting for hypercholesterolemia and neurodegenerative diseases, and pharmacogenomic testing to personalise treatment. Intended users include clinical diagnostic laboratories, hepatologists, and pharmaceutical developers. As the review focuses on biological roles, clinical correlations, and therapeutic potential, these applications remain at an early research stage, requiring translational development and clinical validation before reaching commercial use.

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Abstract

Cytochrome P450 (CYP450) is a group of enzymes that play an essential role in Phase I metabolism, with 57 functional genes classified into 18 families in the human genome, of which the CYP1, CYP2, and CYP3 families are prominent. Beyond drug metabolism, CYP enzymes metabolize endogenous compounds such as lipids, proteins, and hormones to maintain physiological homeostasis. Thus, dysregulation of CYP450 enzymes can lead to different endocrine disorders. Moreover, CYP450 enzymes significantly contribute to fatty acid metabolism, cholesterol synthesis, and bile acid biosynthesis, impacting cellular physiology and disease pathogenesis. Their diverse functions emphasize their therapeutic potential in managing hypercholesterolemia and neurodegenerative diseases. Additionally, CYP450 enzymes are implicated in the onset and development of illnesses such as cancer, influencing chemotherapy outcomes. Assessment of CYP450 enzyme expression and activity aids in evaluating liver health state and differentiating between liver diseases, guiding therapeutic decisions, and optimizing drug efficacy. Understanding the roles of CYP450 enzymes and the clinical effect of their genetic polymorphisms is crucial for developing personalized therapeutic strategies and enhancing drug responses in diverse patient populations.

Research topics

  • Pharmacogenetics and Drug Metabolism
  • Drug Transport and Resistance Mechanisms
  • Liver Disease Diagnosis and Treatment

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DOI: 10.3390/biomedicines12071467

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