| 刘名超,孟青青,崔家华,李绍顺.CYP1B1酶抑制剂的最新研究进展[J].,2017,17(21):4190-4196 |
| CYP1B1酶抑制剂的最新研究进展 |
| Recent Research Progress on the CYP1B1 Inhibitors |
| 投稿时间：2016-10-30 修订日期：2016-11-24 |
| DOI：10.13241/j.cnki.pmb.2017.21.047 |
| 中文关键词: CYP1B1酶抑制剂 肿瘤预防 逆转肿瘤耐药 天然产物 研究进展 |
| 英文关键词: CYP1B1 inhibitors Cancer prevention Overcome drug resistance Natural products Research progress |
| 基金项目:上海市科学技术委员会成果转化项目(12431900602,15431900700)；中国博士后科学基金项目（2014M561479） |
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| 中文摘要: |
| 摘要：细胞色素P450（CYP）1B1是CYP1家族的一个亚型，参与多环芳香烃等前致癌物的代谢活化，并在17-β-雌二醇诱导的乳腺癌发生与发展过程中起到了关键性作用。该酶在肿瘤组织中的特异性高表达及在肿瘤细胞耐药中的作用，也已被大量研究证实。该酶的特异性分布及在肿瘤发生与发展中的重要地位，使得它成为抗肿瘤药物研究中的新靶点。其抑制剂研究，在肿瘤预防及克服肿瘤耐药方面具有重要意义。本文综述了近二十年来发现的CYP1B1酶的强选择性抑制剂，同时分析了它们的构效关系，对发现具有肿瘤预防及逆转肿瘤耐药作用的酶抑制剂提供了理论依据。 |
| 英文摘要: |
| ABSTRACT: CYP1B1 is one member of CYP1 family that could catalyze the bioactivation of procarcinogens such as the polycyclic aromatic hydrocarbons. It is also defined as a key enzyme that takes part in 17-β-estradiol-mediated tumor initiation. Recent knowledge relating to the involvement of CYP1B1 in anticancer drug resistance, the enhanced expression of this enzyme in a variety of human can- cer cells and its pivotal role in the carcinogenic action of 17-β-estradiol, make the inhibition of this enzyme as a new oncological thera- peutic strategy. All of those findings make inhibition of this enzyme as a new method in cancer prevention and therapy of anticancer drug resistance. This review concentrated on the identified CYP1B1 inhibitors in the recent 20 years, which exhibited potent and selective in- hibition on the target enzyme. This work will give great implications for the discovery of new CYP1B1 inhibitors against cancers. |
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