| http://purl.uniprot.org/citations/19047657 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/19047657 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/19047657 | http://www.w3.org/2000/01/rdf-schema#comment | "By using a detergent-washed membrane preparation, the interaction of the fungal natural product inhibitor aureobasidin A (AbA) with inositol phosphorylceramide synthase (IPC synthase) was studied by kinetic analysis of wild-type and mutant enzyme-catalyzed reactions. AbA inhibited the wild-type enzyme from both Candida albicans and Saccharomyces cerevisiae in an irreversible, time-dependent manner, with apparent K(i) values of 183 and 234 pM, respectively. Three synthetic chemistry-derived AbA derivatives, PHA-533179, PHA-556655, and PHA-556656, had affinities 4 to 5 orders of magnitude lower and were reversible inhibitors that competed with the donor substrate phosphatidylinositol (PI). AbA was a reversible, apparently noncompetitive inhibitor, with a K(i) of 1.4 microM, of the IPC synthase from an AbA-resistant S. cerevisiae mutant. The K(m) values for both substrates (ceramide and PI) were similar when they interacted with the mutant and the wild-type enzymes. By contrast, the V(max) for the mutant enzyme was less than 10% of that for the wild-type enzyme. A comparison of the results obtained with AbA with those obtained with two other natural products inhibitors, rustmicin and khafrefungin, revealed that while rustmicin appeared to be a reversible, noncompetitive inhibitor of the wild-type enzyme, with a K(i) of 16.0 nM, khafrefungin had the kinetic properties of a time-dependent inhibitor and an apparent K(i) of 0.43 nM. An evaluation of the efficiencies of these compounds as inhibitors of the mutant enzyme revealed for both a drop in the apparent affinity for the enzyme of more than 2 orders of magnitude."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.org/dc/terms/identifier | "doi:10.1128/aac.00633-08"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.org/dc/terms/identifier | "doi:10.1128/aac.00633-08"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Aeed P.A."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Aeed P.A."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Elhammer A.P."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Elhammer A.P."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Nagiec M.M."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Nagiec M.M."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Young C.L."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/author | "Young C.L."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/date | "2009"xsd:gYear |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/date | "2009"xsd:gYear |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/name | "Antimicrob. Agents Chemother."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/name | "Antimicrob. Agents Chemother."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/pages | "496-504"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/pages | "496-504"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/title | "Inhibition of inositol phosphorylceramide synthase by the cyclic peptide aureobasidin A."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/title | "Inhibition of inositol phosphorylceramide synthase by the cyclic peptide aureobasidin A."xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/volume | "53"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://purl.uniprot.org/core/volume | "53"xsd:string |
| http://purl.uniprot.org/citations/19047657 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/19047657 |
| http://purl.uniprot.org/citations/19047657 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/19047657 |