Shukla Shipra, Yadav Vipin, Mukhopadhyay Gauranga, Prasad Rajendra
Special Centre for Molecular Medicine and Membrane Biology Laboratory, School of Life Sciences, Jawaharlal Nehru University, New Delhi 110067, India.
Eukaryot Cell. 2011 Oct;10(10):1357-66. doi: 10.1128/EC.05041-11. Epub 2011 Aug 19.
We recently demonstrated that CDR1 overexpression in azole-resistant isolates of Candida albicans is due to its enhanced transcriptional activation and increased mRNA stability. In this study, we provide the first evidence of transcriptional regulation of CDR1 by Ncb2, the β subunit of NC2, a heterodimeric regulator of transcription. Conditional NCB2 null mutants displayed decreased susceptibility toward azole and an enhanced transcription of CDR1. Interestingly, Ncb2 associated with the CDR1 promoter under both repression and activation; however, an increase in recruitment was observed under both transient and constitutive activation states. By chromatin immunoprecipitation (ChIP) assay, we showed the preferential recruitment of Ncb2 to the core TATA region under activation (azole-resistant isolate), while under repression (azole-susceptible isolate) it was present at the TATA upstream region. Further, ChIP analysis revealed that Ncb2 binding was not restricted to the CDR1 gene; instead, it was observed on the promoters of genes coregulated with CDR1 by the transcription activator Tac1. The tac1Δ null mutants, which fail to show the drug-induced transient activation of CDR1, also showed no increase in Ncb2 recruitment at the promoter. Taken together, our results show that Ncb2, in conjunction with Tac1, is involved in the transcriptional activation of CDR1, opening up new therapeutic possibilities to combat multidrug resistance (MDR) in C. albicans.
我们最近证明,白色念珠菌唑类耐药菌株中CDR1的过表达是由于其转录激活增强和mRNA稳定性增加。在本研究中,我们首次提供了NC2(一种异二聚体转录调节因子)的β亚基Ncb2对CDR1进行转录调控的证据。条件性NCB2缺失突变体对唑类的敏感性降低,CDR1的转录增强。有趣的是,Ncb2在抑制和激活状态下均与CDR1启动子相关联;然而,在瞬时和组成型激活状态下均观察到募集增加。通过染色质免疫沉淀(ChIP)分析,我们发现Ncb2在激活状态下(唑类耐药菌株)优先募集到核心TATA区域,而在抑制状态下(唑类敏感菌株)它存在于TATA上游区域。此外,ChIP分析表明,Ncb2的结合并不局限于CDR1基因;相反,在转录激活因子Tac1与CDR1共同调控的基因启动子上也观察到了这种结合。tac1Δ缺失突变体未能显示出药物诱导的CDR1瞬时激活,其启动子处的Ncb2募集也未增加。综上所述,我们的结果表明,Ncb2与Tac1一起参与了CDR1的转录激活,为对抗白色念珠菌的多药耐药性(MDR)开辟了新的治疗可能性。