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Plos One : Inhibitor Discovery of Full-length New Delhi Metallo-β- Lactamase-1 Ndm-1, Volume 8

By Dalby, Andrew, R.

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Book Id: WPLBN0003950716
Format Type: PDF eBook :
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Reproduction Date: 2015

Title: Plos One : Inhibitor Discovery of Full-length New Delhi Metallo-β- Lactamase-1 Ndm-1, Volume 8  
Author: Dalby, Andrew, R.
Volume: Volume 8
Language: English
Subject: Journals, Science, Medical Science
Collections: Periodicals: Journal and Magazine Collection (Contemporary)
Historic
Publication Date:
Publisher: Plos

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Dalby, A. R. (n.d.). Plos One : Inhibitor Discovery of Full-length New Delhi Metallo-β- Lactamase-1 Ndm-1, Volume 8. Retrieved from http://new.worldlibrary.net/


Description
Description : New Delhi metallo-b-lactmase-1 (NDM-1) has recently attracted extensive attention for its biological activities to catalyze the hydrolysis of almost all of b-lactam antibiotics. To study the catalytic property of NDM-1, the steady-kinetic parameters of NDM-1 toward several kinds of b-lactam antibiotics have been detected. It could effectively hydrolyze most b-lactams (kcat/ Km ratios between 0.03 to 1.28 mmol21.s21), except aztreonam. We also found that thiophene-carboxylic acid derivatives could inhibit NDM-1 and have shown synergistic antibacterial activity in combination with meropenem. Flexible docking and quantum mechanics (QM) study revealed electrostatic interactions between the sulfur atom of thiophene-carboxylic acid derivatives and the zinc ion of NDM-1, along with hydrogen bond between inhibitor and His189 of NDM-1. The interaction models proposed here can be used in rational design of NDM-1 inhibitors.

 

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