Li Yeqi, Dai Mengyao, Zhang Yuanwei, Lu Ling
Jiangsu Key Laboratory for Microbes and Functional Genomics, Jiangsu Engineering and Technology Research Centre for Microbiology, College of Life Sciences, Nanjing Normal University, Nanjing, China.
Appl Microbiol Biotechnol. 2021 Feb;105(3):1253-1268. doi: 10.1007/s00253-021-11104-5. Epub 2021 Jan 21.
Ergosterol, a major lipid present in the fungal cell membrane, is considered as an effective antifungal drug target. A rational strategy for increasing drug reservoir relies on functionally validation of essential enzymes involved in fungal key biological pathway. Current knowledge regarding the essential genes in the ergosterol biosynthesis pathway is still limited in the opportunistic human pathogen Aspergillus fumigatus. In this study, we characterized two endoplasmic reticulum-localized sterol C-14 reductases encoded by both erg24A and erg24B homologs that are essential for the viability of A. fumigatus despite the fact that neither paralog is essential individually. Loss of one homolog of Erg24 impairs hyphal growth, conidiation, and virulence but has no effect on ergosterol biosynthesis. To investigate the functional significance of erg24, a conditional double mutant (Δerg24B niiA::erg24A) was constructed in the Δerg24B background. Strikingly, the conditional erg24 double mutant exhibited severe growth defects and accumulation of sterol intermediate. Moreover, the addition of metal ions and the overexpression of the corresponding ion transporters could rescue the growth defects of the erg24 double mutant in A. fumigatus, implying that the defective phenotype of the erg24 double mutant is tightly associated with dysregulation of ion homeostasis. Taken together, our results demonstrate the critical role of Erg24 in ergosterol biosynthesis and ion homeostasis in A. fumigatus, which may have important implications for antifungal discovery. KEY POINTS: • We characterized two endoplasmic reticulum-localized sterol C-14 reductases Erg24A and Erg24B in A. fumigatus. • Erg24A and Erg24B in combination, but not individually, are required for the viability of A. fumigatus. • Inactivation of Erg24 leads to the disruption of ion homeostasis and affects ergosterol biosynthesis.
麦角固醇是真菌细胞膜中的一种主要脂质,被认为是一种有效的抗真菌药物靶点。增加药物储备的合理策略依赖于对真菌关键生物学途径中必需酶的功能验证。在机会性人类病原体烟曲霉中,目前关于麦角固醇生物合成途径中必需基因的知识仍然有限。在本研究中,我们鉴定了由erg24A和erg24B同源物编码的两种内质网定位的甾醇C-14还原酶,尽管这两个旁系同源物单独都不是必需的,但它们对烟曲霉的生存能力至关重要。Erg24的一个同源物缺失会损害菌丝生长、分生孢子形成和毒力,但对麦角固醇生物合成没有影响。为了研究erg24的功能意义,在Δerg24B背景下构建了一个条件性双突变体(Δerg24B niiA::erg24A)。令人惊讶的是,条件性erg24双突变体表现出严重的生长缺陷和甾醇中间体的积累。此外,添加金属离子和相应离子转运蛋白的过表达可以挽救烟曲霉中erg24双突变体的生长缺陷,这意味着erg24双突变体的缺陷表型与离子稳态失调密切相关。综上所述,我们的结果证明了Erg24在烟曲霉麦角固醇生物合成和离子稳态中的关键作用,这可能对抗真菌药物的发现具有重要意义。要点:•我们鉴定了烟曲霉中两种内质网定位的甾醇C-14还原酶Erg24A和Erg24B。•烟曲霉的生存能力需要Erg24A和Erg24B共同存在,而非单独存在。•Erg24失活会导致离子稳态破坏并影响麦角固醇生物合成。