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Biochemical characterization of MurF from Streptococcus pneumoniae and the identification of a new MurF inhibitor through ligand-based virtual screening
Turk, Samo (Author), Hrast, Martina (Author), Sosič, Izidor (Author), Barreteau, Hélène (Author), Mengin-Lecreulx, Dominique (Author), Blanot, Didier (Author), Gobec, Stanislav (Author)

URLURL - Presentation file, Visit http://acta.chem-soc.si/60/60-2-294.pdf This link opens in a new window

Abstract
MurF is an essential bacterial enzyme that is involved in the last intracellular stage of peptidoglycan biosynthesis, and therefore it has the potential to be exploited as a target for the development of new antibacterials. Here, we report on the expression, purification and biochemical characterization of MurF from an important pathogen, Streptococcus pneumoniae. Additionally, ligand-based virtual screening was successfully used and a new hit compound with micromolar inhibitory activities against MurF enzymes from S. pneumoniae and Escherichia coli was identified.

Language:English
Keywords:MurF, peptidoglikani, Streptococcus pneumoniae, virtualno rešetanje, protibakterijske učinkovine, Escherichia coli, zaviralna aktivnost
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Year:2013
Number of pages:str. 294-299
Numbering:Vol. 60, no. 2
UDC:542+543.057
ISSN on article:1318-0207
COBISS.SI-ID:3477105 Link is opened in a new window
Views:386
Downloads:94
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Record is a part of a journal

Title:Acta chimica slovenica
Shortened title:Acta chim. slov.
Publisher:Slovensko kemijsko društvo, =Slovenian Chemical Society
ISSN:1318-0207
COBISS.SI-ID:14086149 This link opens in a new window

Secondary language

Language:English
Abstract:
MurF je esencialen bakterijski encim, ki sodeluje pri zadnji znotrajcelični stopnji biosinteze peptidoglikana in je kot tak obetavna tarča za razvoj novihprotibakterijskih učinkovin. V tem prispevku poročamo o uspešni ekspresiji, izolaciji in biokemijski karakterizaciji encima MurF iz pomembnega patogenega seva Streptococcus pneumoniae. Poleg tega smo tudi uspešno uporabili virtualno rešetanje na osnovi liganda in odkrili novo spojino zadetek z zaviralno aktivnostjo v mikromolarnem območju na encima MurFiz S. pneumoniae in Escherichia coli.


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