Decker H, Zähner H, Heitsch H, König W A, Fiedler H P
Universität Tübingen, Biologisches Institut, Tübingen, FRG.
J Gen Microbiol. 1991 Aug;137(8):1805-13. doi: 10.1099/00221287-137-8-1805.
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 [Km = 24 microM, Vmax = 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.
研究了不同多氧霉素的构效关系，以评估强效几丁质合酶抑制剂的结构要求。我们研究了多氧霉素通过解脂耶氏酵母的肽转运系统的转运情况，并确定了多氧霉素Z摄取的动力学参数[Km = 24 microM，Vmax = 2.2 nmol min-1 (mg干重)-1]。我们证明了二肽多氧霉素N端氨基酸的β-甲基基团可保护该分子免受不同真菌粗细胞提取物中肽酶活性的影响。此外，还讨论了几丁质合酶抑制常数、多氧霉素通过肽转运系统的转运、对细胞蛋白酶降解的敏感性以及多氧霉素全细胞活性之间的关系。
