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https://hdl.handle.net/2440/92379
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Type: | Journal article |
Title: | Improved synthesis of biotinol-5'-AMP: implications for antibacterial discovery |
Author: | Tieu, W. Polyak, S. Paparella, A. Yap, M. Soares Da Costa, T. Ng, B. Wang, G. Lumb, R. Bell, J. Turnidge, J. Wilce, M. Booker, G. Abell, A. |
Citation: | ACS Medicinal Chemistry Letters, 2015; 6(2):216-220 |
Publisher: | American Chemical Society |
Issue Date: | 2015 |
ISSN: | 1948-5875 1948-5875 |
Statement of Responsibility: | William Tieu, Steven W. Polyak, Ashleigh S. Paparella, Min Y. Yap, Tatiana P. Soares da Costa, Belinda Ng, Geqing Wang, Richard Lumb, Jan M. Bell, John D. Turnidge, Matthew C. J. Wilce, Grant W. Booker, and Andrew D. Abell |
Abstract: | An improved synthesis of biotinol-5'-AMP, an acyl-AMP mimic of the natural reaction intermediate of biotin protein ligase (BPL), is reported. This compound was shown to be a pan inhibitor of BPLs from a series of clinically important bacteria, particularly Staphylococcus aureus and Mycobacterium tuberculosis, and kinetic analysis revealed it to be competitive against the substrate biotin. Biotinol-5'-AMP also exhibits antibacterial activity against a panel of clinical isolates of S. aureus and M. tuberculosis with MIC values of 1-8 and 0.5-2.5 μg/mL, respectively, while being devoid of cytotoxicity to human HepG2 cells. |
Keywords: | Antibiotics enzyme inhibitors biotin protein ligase chemical synthesis drug design |
Rights: | Copyright © 2014 American Chemical Society |
DOI: | 10.1021/ml500475n |
Grant ID: | http://purl.org/au-research/grants/nhmrc/1011806 http://purl.org/au-research/grants/nhmrc/1068885 |
Published version: | http://dx.doi.org/10.1021/ml500475n |
Appears in Collections: | Aurora harvest 2 IPAS publications |
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