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Irreversible Inhibition of Metallo‐β‐lactamase (IMP‐1) by 3‐(3‐Mercaptopropionylsulfanyl)propionic Acid Pentafluorophenyl Ester
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Citations
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References
2005
Year
Covalent Amide BondMolecular BiologyAntibiotic ResistanceTitle CompoundBacterial PathogensPharmaceutical ChemistryDrug ResistanceMedicinal ChemistryAntimicrobial ResistanceAntimicrobial Drug DiscoveryDrug Resistance AnalysisBiochemistryIrreversible InhibitionLys 224Antibacterial AgentAntimicrobial CompoundPharmacologyBacterial ResistanceAntimicrobial Resistance GeneAntibioticsNatural SciencesMicrobiologyMedicineDrug Discovery
Resistance is futile: Pathogenic bacteria that produce metallo-β-lactamases are recognized as a serious threat because of their resistance to antibiotics. The title compound has now been shown to be an irreversible inhibitor for a metallo-β-lactamase (IMP-1). The X-ray crystallographic structure (see picture) has revealed that the inhibitor binds to IMP-1 with formation of a covalent amide bond with the amino group (Nζ) of Lys 224. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2005/z500835_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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