Penicillin-binding proteins: evergreen drug targets

Highlights • Structures of sensitive and resistant variants of essential penicillin-binding proteins (PBPs). • Spectroscopic studies of the reaction of essential PBPs with β-lactams. • Novel, non-β-lactam covalent inhibitors that have the potential to overcome PBP mediated β-lactam resistance. • Non...

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Bibliographic Details
Published in:	Current opinion in pharmacology Vol. 18; pp. 112 - 119
Main Authors:	Frère, Jean-Marie, Page, Malcolm GP
Format:	Journal Article Web Resource
Language:	English
Published:	England Elsevier Ltd 01-10-2014 Elsevier
Subjects:	Anti-Bacterial Agents - pharmacology beta-Lactams - pharmacology Biochemistry, biophysics & molecular biology Biochimie, biophysique & biologie moléculaire Internal Medicine Life sciences Medical Education Penicillin Resistance - physiology Penicillin-Binding Proteins - antagonists & inhibitors Penicillin-Binding Proteins - chemistry Penicillin-Binding Proteins - metabolism Penicillin-Binding Proteins/antagonists & inhibitors/chemistry/metabolism Protein Conformation Sciences du vivant
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Summary:	Highlights • Structures of sensitive and resistant variants of essential penicillin-binding proteins (PBPs). • Spectroscopic studies of the reaction of essential PBPs with β-lactams. • Novel, non-β-lactam covalent inhibitors that have the potential to overcome PBP mediated β-lactam resistance. • Non-covalent, tight-binding inhibitors with potentially new mechanisms of action and demonstrable antibiotic activity.
Bibliography:	ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-3 content type line 23 ObjectType-Review-1 scopus-id:2-s2.0-84908279514
ISSN:	1471-4892 1471-4973 1471-4973
DOI:	10.1016/j.coph.2014.09.012