Cytochrome P450s in the development of target-based anticancer drugs

作者: Kedar Purnapatre , Sunil K. Khattar , Kulvinder Singh Saini

DOI: 10.1016/J.CANLET.2007.10.024

关键词:

摘要: Enzymes of the cytochrome P450 (CYP) superfamily are major determinants half-life and execute pharmacological effects many therapeutic drugs. In new drug discovery research, recombinant (human) CYPs also used for identifying active or inactive metabolites that could lead to increased potency toxicity a molecule. addition, CYP inhibition by anticancer drugs might adverse reactions, multiple-drug resistance, drug-drug interactions. During pre-clinical evaluation New Chemical Entity (NCE), large amounts purified required studying metabolism pharmacokinetic parameters. Therefore, present research efforts focused over-express these human in bacteria, yeast, insect mammalian cells, followed their purification on an industrial scale facilitate identification novel This review summarizes merits limitations expression systems optimized production individual isoforms, usefulness development target-based, safe efficacious NCEs treatment cancer.

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