About: Bismuth antimicrobial drugs serve as broad-spectrum metallo-β-lactamase inhibitors

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About: Bismuth antimicrobial drugs serve as broad-spectrum metallo-β-lactamase inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Bismuth antimicrobial drugs serve as broad-spectrum metallo-β-lactamase inhibitors
Creator	Chiu-Yat Woo, Patrick Li, Hongyan Sun, Hongzhe Ho, Pak-Leung Gao, Peng Lai, Tsz-Pui Ma, Guixing Wang, Runming Zhang, Hongmin Kao, Yi-Tsun Kong, Hong Zhang, Gao, Hongmin Kong, Kong, Pok Lai, Peng Lam, Fu Lam, Hong Wang, Tsz-Pui
Source	PMC
abstract	Drug-resistant superbugs pose a huge threat to human health. Infections by Enterobacteriaceae producing metallo-β-lactamases (MBLs), e.g., New Delhi metallo-β-lactamase 1 (NDM-1) are very difficult to treat. Development of effective MBL inhibitors to revive the efficacy of existing antibiotics is highly desirable. However, such inhibitors are not clinically available till now. Here we show that an anti-Helicobacter pylori drug, colloidal bismuth subcitrate (CBS), and related Bi(III) compounds irreversibly inhibit different types of MBLs via the mechanism, with one Bi(III) displacing two Zn(II) ions as revealed by X-ray crystallography, leading to the release of Zn(II) cofactors. CBS restores meropenem (MER) efficacy against MBL-positive bacteria in vitro, and in mice infection model, importantly, also slows down the development of higher-level resistance in NDM-1-positive bacteria. This study demonstrates a high potential of Bi(III) compounds as the first broad-spectrum B1 MBL inhibitors to treat MBL-positive bacterial infection in conjunction with existing carbapenems.
has issue date	2018-01-30(xsd:dateTime)
bibo:doi	10.1038/s41467-018-02828-6
bibo:pmid	29382822
has license	cc-by
sha1sum (hex)	49e1868b232e6ec98ae7cbc0745613925205e056
schema:url	https://doi.org/10.1038/s41467-018-02828-6
resource representing a document's title	Bismuth antimicrobial drugs serve as broad-spectrum metallo-β-lactamase inhibitors
has PubMed Central identifier	PMC5789847
has PubMed identifier	29382822
schema:publication	Nat Commun
resource representing a document's body	covid:49e1868b232e6ec98ae7cbc0745613925205e056#body_text
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