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Antibiotics 2014, 3(2), 128-142; doi:10.3390/antibiotics3020128

Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

Department of Chemistry, American University, 4400 Massachusetts Ave. NW, Washington, DC, 20016-8014, USA
Received: 31 December 2013 / Revised: 24 February 2014 / Accepted: 25 February 2014 / Published: 3 April 2014
(This article belongs to the Special Issue Mechanisms of Antibiotic Resistance)
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The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets.
Keywords: antibiotic resistance; directed evolution; β-lactams as chemical probes antibiotic resistance; directed evolution; β-lactams as chemical probes
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Konaklieva, M.I. Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects. Antibiotics 2014, 3, 128-142.

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