Paul Sanjoy, Schmidt Jennifer A, Moye-Rowley W Scott
Department of Molecular Physiology and Biophysics, Carver College of Medicine, 6-530 Bowen Science Bldg., University of Iowa, Iowa City, IA 52242, USA.
Eukaryot Cell. 2011 Feb;10(2):187-97. doi: 10.1128/EC.00277-10. Epub 2010 Dec 3.
Candida glabrata is an opportunistic human pathogen that is increasingly associated with candidemia, owing in part to the intrinsic and acquired high tolerance the organism exhibits for the important clinical antifungal drug fluconazole. This elevated fluconazole resistance often develops through gain-of-function mutations in the zinc cluster-containing transcriptional regulator C. glabrata Pdr1 (CgPdr1). CgPdr1 induces the expression of an ATP-binding cassette (ABC) transporter-encoding gene, CgCDR1. Saccharomyces cerevisiae has two CgPdr1 homologues called ScPdr1 and ScPdr3. These factors control the expression of an ABC transporter-encoding gene called ScPDR5, which encodes a homologue of CgCDR1. Loss of the mitochondrial genome (ρ(0) cell) or overexpression of the mitochondrial enzyme ScPsd1 induces ScPDR5 expression in a strictly ScPdr3-dependent fashion. ScPdr3 requires the presence of a transcriptional Mediator subunit called Gal11 (Med15) to fully induce ScPDR5 transcription in response to ρ(0) signaling. ScPdr1 does not respond to either ρ(0) signals or ScPsd1 overproduction. In this study, we employed transcriptional fusions between CgPdr1 target promoters, like CgCDR1, to demonstrate that CgPdr1 stimulates gene expression via binding to elements called pleiotropic drug response elements (PDREs). Deletion mapping and electrophoretic mobility shift assays demonstrated that a single PDRE in the CgCDR1 promoter was capable of supporting ρ(0)-induced gene expression. Removal of one of the two ScGal11 homologues from C. glabrata caused a major defect in drug-induced expression of CgCDR1 but had a quantitatively minor effect on ρ(0)-stimulated transcription. These data demonstrate that CgPdr1 appears to combine features of ScPdr1 and ScPdr3 to produce a transcription factor with chimeric regulatory properties.
光滑念珠菌是一种机会性人类病原体,越来越多地与念珠菌血症相关,部分原因是该生物体对重要的临床抗真菌药物氟康唑表现出内在的和获得性的高耐受性。这种对氟康唑的抗性升高通常是通过含锌簇转录调节因子光滑念珠菌Pdr1(CgPdr1)的功能获得性突变而产生的。CgPdr1诱导编码ATP结合盒(ABC)转运蛋白的基因CgCDR1的表达。酿酒酵母有两个CgPdr1同源物,称为ScPdr1和ScPdr3。这些因子控制编码ABC转运蛋白的基因ScPDR5的表达,ScPDR5编码CgCDR1的同源物。线粒体基因组缺失(ρ(0)细胞)或线粒体酶ScPsd1的过表达以严格依赖ScPdr3的方式诱导ScPDR5表达。ScPdr3需要一种称为Gal11(Med15)的转录中介亚基的存在,以响应ρ(0)信号充分诱导ScPDR5转录。ScPdr1对ρ(0)信号或ScPsd1的过量产生均无反应。在本研究中,我们利用CgPdr1靶启动子(如CgCDR1)之间的转录融合,证明CgPdr1通过与称为多药耐药反应元件(PDRE)的元件结合来刺激基因表达。缺失定位和电泳迁移率变动分析表明,CgCDR1启动子中的单个PDRE能够支持ρ(0)诱导的基因表达。从光滑念珠菌中去除两个ScGal11同源物之一会导致药物诱导的CgCDR1表达出现重大缺陷,但对ρ(0)刺激的转录产生的定量影响较小。这些数据表明,CgPdr1似乎结合了ScPdr1和ScPdr3的特征,产生了一种具有嵌合调节特性的转录因子。