STRUCTURE-ACTIVITY-RELATIONSHIPS OF THE NIKKOMYCINS
STRUCTURE-ACTIVITY-RELATIONSHIPS OF THE NIKKOMYCINS
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DOI：
10.1099/00221287-137-8-1805
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发表时间：
1991-08-01
期刊：
影响因子：
--
通讯作者：
FIEDLER, HP
中科院分区：
文献类型：
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作者：
DECKER, H;ZAHNER, H;FIEDLER, HP
研究了不同尼可霉素的构效关系，以评估对有效的甲壳素合成酶抑制剂的结构要求。我们研究了尼可霉素通过解脂雅罗维菌酵母肽转运系统的转运，测定了尼可霉素Z摄取的动力学参数[K(M)=24-mU-M，V(Max)=2.2nmolmin-1(mg干重)-1]。我们证明了N端氨基酸的β-甲基对不同真菌细胞粗提物中的肽酶活性有保护作用。此外，还讨论了几丁质合成酶的抑制常数、尼可霉素通过肽转运系统的转运、对细胞蛋白酶降解的敏感性和尼可霉素的全细胞活性之间的关系。
The structure-activity relationships of different nikkomycins were studied to evaluate the structural requirements for a potent chitin synthase inhibitor. We investigated the transport of the nikkomycins via the peptide transport system of the yeast Yarrowia lipolytica and determined the kinetic parameters for nikkomycin Z uptake [K(m) = 24-mu-M, V(max) = 2.2 nmol min-1 (mg dry wt)-1]. We demonstrated that the beta-methyl group of the N-terminal amino acid of dipeptide nikkomycins protects the molecule against peptidase activity in crude cell-extracts of different fungi. Furthermore, the relationship between inhibition constants for chitin synthase, transport of the nikkomycins via the peptide transport system, susceptibility to degradation by cellular proteases and whole-cell activity of the nikkomycins are discussed.