Chen Yakun, Nie Daotai
Department of Medical Microbiology, Immunology and Cell Biology, Southern Illinois University, School of Medicine and SimmonsCooper Cancer Institute, Springfield, IL 62794-9626, USA.
Recent Pat Anticancer Drug Discov. 2009 Jan;4(1):19-27. doi: 10.2174/157489209787002498.
Multi-drug resistance (MDR) is a significant barrier to effective chemotherapy of cancer. The induction of drug metabolizing enzymes (DMEs) and efflux transporters has been regarded as one of the major mechanisms of drug resistance. As a master transcription factor of DMEs and efflux transporters, pregnane X receptor (PXR), an orphan nuclear receptor known for its activation by structurally diverse compounds, is expressed in some cancer cells and tissues, and is implicated as a novel master regulator of MDR in cancers. This review describes recent publications and patents on the mechanism of PXR transcription, the expression of PXR in cancers, and its potential roles in cancer MDR. We also discuss the recent patents published to overcome PXR-mediated MDR and other potential roles of PXR in cancers.
多药耐药（MDR）是癌症有效化疗的重大障碍。药物代谢酶（DMEs）和外排转运蛋白的诱导被认为是耐药的主要机制之一。作为DMEs和外排转运蛋白的主要转录因子，孕烷X受体（PXR）是一种孤儿核受体，因其能被结构多样的化合物激活而闻名，在一些癌细胞和组织中表达，并被认为是癌症中MDR的一种新型主要调节因子。本综述描述了近期关于PXR转录机制、PXR在癌症中的表达及其在癌症MDR中的潜在作用的出版物和专利。我们还讨论了为克服PXR介导的MDR而发表的近期专利以及PXR在癌症中的其他潜在作用。
