Abstract
Human cytochrome P450 (CYP) enzymes, as membrane-bound hemoproteins, play important roles in the detoxification of drugs, cellular metabolism, and homeostasis. In humans, almost 80% of oxidative metabolism and approximately 50% of the overall elimination of common clinical drugs can be attributed to one or more of the various CYPs, from the CYP families 1–3. In addition to the basic metabolic effects for elimination, CYPs are also capable of affecting drug responses by influencing drug action, safety, bioavailability, and drug resistance through metabolism, in both metabolic organs and local sites of action. Structures of CYPs have recently provided new insights into both understanding the mechanisms of drug metabolism and exploiting CYPs as drug targets. Genetic polymorphisms and epigenetic changes in CYP genes and environmental factors may be responsible for interethnic and interindividual variations in the therapeutic efficacy of drugs. In this review, we summarize and highlight the structural knowledge about CYPs and the major CYPs in drug metabolism. Additionally, genetic and epigenetic factors, as well as several intrinsic and extrinsic factors that contribute to interindividual variation in drug response are also reviewed, to reveal the multifarious and important roles of CYP-mediated metabolism and elimination in drug therapy.
Highlights
Drug metabolism is the process of altering their molecules chemically after entering the body [1]
This is an important progress for drug metabolism, because the lipophilic nature of drugs can keep them staying for longer in the body, which may in turn lead to toxicity [4,5]
cytochrome P450 (CYP) play important roles in the maintenance of general human health, as they relate to the metabolism of pharmaceuticals
Summary
Drug metabolism is the process of altering their molecules chemically after entering the body [1]. The majority of drugs lipophilic centers are converted to hydrophilic centers during drug biotransformation, which can increase their water solubility, to allow elimination in urine or bile [3]. This is an important progress for drug metabolism, because the lipophilic nature of drugs can keep them staying for longer in the body, which may in turn lead to toxicity [4,5]. We outline the clinical implications and therapeutic benefits of CYPs. With advances in molecular biology and biochemical technology, our knowledge of these critical metabolic process will eventually assist in the development of individualized pharmacotherapy, avoiding harmful adverse drug reactions or treatment failures
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