Structure-activity relationships of the nikkomycins
Open Access
- 1 August 1991
- journal article
- Published by Microbiology Society in Journal of General Microbiology
- Vol. 137 (8) , 1805-1813
- https://doi.org/10.1099/00221287-137-8-1805
Abstract
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 µM, Vmax = 2.2 nmol min-1 (mg dry wt)-1]. We demonstrated that the β-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.Keywords
This publication has 0 references indexed in Scilit: