Department of Molecular Biology and Microbiology, Tufts University, 136 Harrison Ave, Boston, MA, 02111, USA.
Mol Genet Genomics. 2011 Dec;286(5-6):347-57. doi: 10.1007/s00438-011-0650-z. Epub 2011 Oct 5.
In the opportunistic fungal pathogen Candida albicans, up-regulation of MDR1, encoding an efflux transporter, leads to increased resistance to the antifungal drug fluconazole. Antifungal resistance has been linked to several types of genetic change in C. albicans, including changes in genome structure, genetic alteration of the drug target, and overexpression of transporters. High-level over-expression of MDR1 is commonly mediated by mutation in a trans-acting factor, Mrr1p. This report describes a second mechanism that contributes to up-regulation of MDR1 expression. By analyzing the sequence of the MDR1 promoter region in fluconazole-resistant and fluconazole-susceptible strains, we identified sequence polymorphisms that defined two linkage groups, corresponding to the two alleles in the diploid genome. One of the alleles conferred higher MDR1 expression compared with the other allele. Strains in which both alleles were of the higher activity type were common in collections of clinically isolated strains while strains carrying only the less active allele were rare. As increased expression of MDR1 confers higher resistance to drugs, strains with the more active MDR1 promoter allele may grow or survive longer when exposed to drugs or other selective pressures, providing greater opportunity for mutations that confer high-level drug resistance to arise. Through this mechanism, higher activity alleles of the MDR1 promoter could promote the development of drug resistance.
在机会性真菌病原体白色念珠菌中,MDR1 的上调导致对抗真菌药物氟康唑的耐药性增加。MDR1 编码一种外排转运蛋白,其表达的增加与白色念珠菌中几种类型的遗传变化有关,包括基因组结构的改变、药物靶标遗传改变和转运蛋白的过表达。MDR1 的高水平过表达通常是由一个反式作用因子 Mrr1p 的突变介导的。本报告描述了第二个导致 MDR1 表达上调的机制。通过分析氟康唑耐药和氟康唑敏感株中 MDR1 启动子区的序列,我们鉴定出了序列多态性,这些多态性定义了两个连锁群,对应于二倍体基因组中的两个等位基因。其中一个等位基因与另一个等位基因相比,MDR1 表达更高。在临床分离株的集合中,具有两种等位基因的高活性类型的菌株很常见,而仅携带低活性等位基因的菌株则很少见。由于 MDR1 的表达增加赋予了更高的耐药性,因此当暴露于药物或其他选择性压力时,具有更高活性 MDR1 启动子等位基因的菌株可能会更长时间地生长或存活,从而有更多机会产生赋予高水平耐药性的突变。通过这种机制,MDR1 启动子的高活性等位基因可能会促进耐药性的发展。