title: Anticandidal properties of N-acylpeptides containing an inhibitor of glucosamine-6-phosphate synthase.
abstract: A series of N-acyl peptides 1-9, containing an inhibitor of glucosamine-6-phosphate synthase have been synthesised and tested against Candida strains. N-Acylated peptides inhibit glucosamine-6-phosphate synthase in cell free extracts from Candida albicans. Antifungal activities of the tested compounds correlated with their lipophilic properties. Peptides acylated with decanoic acid were found to be the most potent in the series. N-decanoylpeptides also showed activity against Candida albicans Gu5 resistant mutant with Cdr1 and Cdr2 drug extrusion proteins that causes MDR by an active efflux mechanism.
authors.affiliation: Department of Pharmaceutical Technology and Biochemistry, Gdańsk University of Technology, 11/12 Narutowicza Street, 80-952 Gdańsk, Poland. ryszarda@chem.pg.gda.pl
authors.forename: Ryszard
authors.initials: R
authors.lastname: Andruszkiewicz
authors.forename: Teresa
authors.initials: T
authors.lastname: Zieniawa
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Walkowiak
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000378:metabolism*; D002177:Candidiasis / Q000188:drug therapy*; D002474:Cell-Free System; D002851:Chromatography, High Pressure Liquid; D004353:Drug Evaluation, Preclinical; D025141:Drug Resistance, Fungal; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D005945:Glutamine-Fructose-6-Phosphate Transaminase (Isomerizing) / Q000037:antagonists & inhibitors*; D018922:HL-60 Cells; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D009154:Mutation; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D004791:Enzyme Inhibitors; D010455:Peptides; D005945:Glutamine-Fructose-6-Phosphate Transaminase (Isomerizing)