| Development of screening assays and discovery of initial inhibitors of pneumococcal peptidoglycan deacetylase PgdA. | |
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MedLine Citation:
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PMID: 21501597 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The essential cell wall peptidoglycan is the target of several components of the innate immune system and its disruption results in lysis of invading bacteria. The pathogen Streptococcus pneumoniae produces a peptidoglycan N-acetylglucosamine deacetylase, PgdA, to modify the peptidoglycan structure. The activity of PgdA contributes to the bacteria's resistance to lysozyme, which is an important antimicrobial factor of the human innate immune system. In this study we report on the activity of PgdA against natural and artificial substrates. We have also established a virtual high-throughput screening and a new enzyme assay to search for compounds inhibiting PgdA. Two compounds with IC(50) values in the micromolar range have been identified and they could serve as leads for the search of inhibitors of PgdA, an important pneumococcal virulence factor. |
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Authors:
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Nhat Khai Bui; Samo Turk; Stephan Buckenmaier; Flint Stevenson-Jones; Benjamin Zeuch; Stanislav Gobec; Waldemar Vollmer |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-4-8 |
Journal Detail:
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Title: Biochemical pharmacology Volume: - ISSN: 1873-2968 ISO Abbreviation: - Publication Date: 2011 Apr |
Date Detail:
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Created Date: 2011-4-19 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0101032 Medline TA: Biochem Pharmacol Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Inc. All rights reserved. |
Affiliation:
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Centre for Bacterial Cell Biology, Institute for Cell and Molecular Biosciences, Newcastle University, Richardson Road, Newcastle upon Tyne NE2 4AX, United Kingdom. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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