期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 24, 期 18, 页码 4406-4409出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2016.07.035
关键词
Carbonic anhydrase; Boronic acid; Bortezomib; Pathogenic fungi; Pathogenic bacteria; Drosophila melanogaster
资金
- European Union
Inhibition of the beta-carbonic anhydrases (CAs, EC 4.2.1.1) from pathogenic fungi (Cryptococcus neoformans, Candida albicans, Candida glabrata, Malassezia globosa) and bacteria (three isoforms from Mycobacterium tuberculosis, Rv3273, Rv1284 and Rv3588), as well from the insect Drosophila melanogaster (DmeCA) and the plant Flaveria bidentis (FbiCA1) with the boronic acid peptidomimetic proteosome inhibitor bortezomib was investigated. Bortezomib was a micromolar inhibitor of all these enzymes, with K(I)s ranging between 1.12 and 11.30 mu M. Based on recent crystallographic data it is hypothesized that the B(OH)(2) moiety of the inhibitor is directly coordinated to the zinc ion from the enzyme active site. The class of boronic acids, an under-investigated type of CA inhibitors, may lead to the development of anti-infectives with a novel mechanism of action, based on the pathogenic organisms CA inhibition. (C) 2016 Elsevier Ltd. All rights reserved.
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