Rogers K M, Pierson C A, Culbertson N T, Mo C, Sturm A M, Eckstein J, Barbuch R, Lees N D, Bard M
Department of Biology, Indiana University Purdue University Indianapolis, West Michigan St., Indianapolis, IN 46202-5132, USA.
Antimicrob Agents Chemother. 2004 Sep;48(9):3425-35. doi: 10.1128/AAC.48.9.3425-3435.2004.
Sterol synthesis in fungi is an aerobic process requiring molecular oxygen and, for several cytochrome-mediated reactions, aerobically synthesized heme. Cytochrome b(5) is required for sterol C5-6 desaturation and the encoding gene, CYB5, is nonessential in Saccharomyces cerevisiae. Cyb5p and Ncp1p (cytochrome P-450 reductase) appear to have overlapping functions in this organism, with disruptions of each alone being viable. The cytochrome P-450 reductase phenotype has also been shown to demonstrate increased sensitivity to azole antifungals. Based on this phenotype, the CYB5 gene in the human pathogen Candida albicans was investigated to determine whether the cyb5 genotype was viable and would also demonstrate azole sensitivity. Sequential disruption of the CYB5 alleles by direct transformation resulted in viability, presumably conferred by the presence of a third copy of the CYB5 gene. Subsequent disruption procedures with a pMAL2-CYB5 rescue cassette and a CYB5-URA3 blaster cassette resulted in viable cyb5 strains with no third copy. The C. albicans CYB5 gene is concluded to be nonessential. Thus, the essentiality of this gene and whether we observed two or three alleles was dependent upon the gene disruption protocol. The C. albicans cyb5 strains produced a sterol profile containing low ergosterol levels and sterol intermediates similar to that reported for the S. cerevisiae cyb5. The C. albicans cyb5 shows increased sensitivity to azoles and terbinafine, an inhibitor of squalene epoxidase, and, unexpectedly, increased resistance to morpholines, which inhibit the ERG2 and ERG24 gene products. These results indicate that an inhibitor of Cyb5p would not be lethal but would make the cell significantly more sensitive to azole treatment.
真菌中的甾醇合成是一个需氧过程,需要分子氧,并且对于几个细胞色素介导的反应而言,还需要有氧合成的血红素。细胞色素b(5)是甾醇C5-6去饱和所必需的,其编码基因CYB5在酿酒酵母中并非必需。在这种生物体中,Cyb5p和Ncp1p(细胞色素P-450还原酶)似乎具有重叠功能,单独破坏其中任何一个都是可行的。细胞色素P-450还原酶表型也已被证明对唑类抗真菌药表现出更高的敏感性。基于这种表型,对人类病原体白色念珠菌中的CYB5基因进行了研究,以确定cyb5基因型是否可行,以及是否也会表现出对唑类的敏感性。通过直接转化对CYB5等位基因进行连续破坏导致了菌株存活,推测这是由CYB5基因的第三个拷贝的存在所赋予的。随后用pMAL2-CYB5拯救盒和CYB5-URA3破坏盒进行的破坏程序产生了没有第三个拷贝的可行cyb5菌株。得出结论,白色念珠菌的CYB5基因并非必需。因此,该基因的必需性以及我们观察到的是两个还是三个等位基因取决于基因破坏方案。白色念珠菌的cyb5菌株产生的甾醇谱中麦角甾醇水平较低,且甾醇中间体与酿酒酵母cyb5中报道的相似。白色念珠菌的cyb5对唑类和特比萘芬(一种角鲨烯环氧酶抑制剂)表现出更高的敏感性,并且出乎意料的是,对抑制ERG2和ERG24基因产物的吗啉类表现出更高的抗性。这些结果表明,Cyb5p的抑制剂不会致死,但会使细胞对唑类治疗显著更敏感。