药物代谢酶在癌症与癌症治疗中的作用。

Role of Drug-metabolizing Enzymes in Cancer and Cancer Therapy.

机构信息

Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China; Co-innovation Center of Henan Province for New Drug R & D and Preclinical Safety; School of Pharmaceutical Sciences; Institute of Drug Discovery and Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan 450001, China.

出版信息

Curr Drug Metab. 2020;21(1):67-76. doi: 10.2174/1389200221666200103111053.

DOI:10.2174/1389200221666200103111053

PMID:31902352

Abstract

BACKGROUND

Cancer is one of the most serious diseases threatening human health with high morbidity and mortality in the world. For the treatment of cancer, chemotherapy is one of the most widely used strategies, for almost all kinds of tumors and diverse stages of tumor development. The efficacy of chemotherapy not only depends on the activity of the drug administrated but also on whether the compound could reach the effective therapeutic concentration in tumor cells. Therefore, expression and activity of drug-metabolizing enzymes (DMEs) in tumor tissues and metabolic organs of cancer patients are important for the dispositional behavior of anticancer drugs as well as the clinical response of chemotherapy.

METHODS

This review summarizes the recent advancement of the DMEs expression and activity in various cancers, as well as the potential regulatory mechanisms of major DMEs in cancer and cancer therapy.

RESULTS

Compared to normal tissues, expression and activity of major DMEs are significantly dysregulated in patients by various factors including epigenetic modification, ligand-activated transcriptional regulation and signaling pathways. Additionally, DMEs play an important role in anticancer drug efficacy, chemoresistance as well as the activation of prodrugs.

CONCLUSION

This review reinforces a more comprehensive understanding of DMEs in cancer and cancer therapy, and provides more opportunities for cancer therapy.

摘要

背景

癌症是威胁人类健康的最严重疾病之一，在世界范围内具有高发病率和死亡率。对于癌症的治疗，化疗是最广泛使用的策略之一，几乎适用于所有类型的肿瘤和不同阶段的肿瘤发展。化疗的疗效不仅取决于给药药物的活性，还取决于化合物是否能在肿瘤细胞中达到有效的治疗浓度。因此，癌症患者肿瘤组织和代谢器官中药物代谢酶（DMEs）的表达和活性对于抗癌药物的处置行为以及化疗的临床反应很重要。