Chaxamycins A-D, Bioactive Ansamycins from a Hyper-arid Desert Streptomyces sp.

Rateb, Mostafa E. and Houssen, Wael E. and Arnold, Markus and Abdelrahman, Mostafa H. and Deng, Hai and Harrison, William T. A. and Okoro, Chinyere K. and Asenjo, Juan A. and Andrews, Barbara A. and Ferguson, Gail and Bull, Alan T. and Goodfellow, Michael and Ebel, Rainer and Jaspars, Marcel (2011) Chaxamycins A-D, Bioactive Ansamycins from a Hyper-arid Desert Streptomyces sp. Journal of Natural Products, 74 (6). pp. 1491-1499. ISSN 1520-6025. (The full text of this publication is not available from this repository)

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Official URL
http://dx.doi.org/10.1021/np200320u

Abstract

Streptomyces sp. strain C34, isolated from soil collected in the Chilean hyper-arid Atacama Desert, was cultured on different media, resulting in the isolation and identification of four new ansamycin-type polyketides. The organism was selected for chemical investigation on the basis of a genome-mining PCR-based experiment targeting the gene encoding rifamycin-specific 3-amino-5-hydroxybenzoic acid synthetase (AHBA). The isolated compounds were structurally characterized using NMR and MS techniques and named chaxamycins A-D (1-4). Compounds 1-4 were tested for their antibacterial activity against Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 25922 and for their ability to inhibit the intrinsic ATPase activity of the heat shock protein 90 (Hsp90). Chaxamycin D (4), which showed a selective antibacterial activity against S. aureus ATCC 25923, was tested further against a panel of MRSA clinical isolates. In a virtual screening experiment, chaxamycins A-D (1-4) have also been docked into the ATP-binding pocket in the N-terminal domain of the Hsp90, and the observed interactions are discussed.

Item Type: Article
Subjects: Q Science
Divisions: Faculties > Science Technology and Medical Studies > School of Biosciences
Faculties > Science Technology and Medical Studies > School of Biosciences > Biomedical Research Group
Depositing User: Sue Davies
Date Deposited: 11 Nov 2011 16:19
Last Modified: 29 Apr 2014 15:22
Resource URI: http://kar.kent.ac.uk/id/eprint/27994 (The current URI for this page, for reference purposes)
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