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Understanding the cross-talk between the selected residues of beta-lactamase/Bla
β-Lactam antibiotics inhibit bacterial cell wall synthesis and thus cause cell death. Production of β-lactamase is one of the mechanisms that confer resistance to bacteria. The most effective way to counteract the emergence of β-lactamases, which hydrolyse the β-lactam ring of the antibiotics, is the administration of the antibiotic in combination with β-lactamase inhibitors such as clavulanic acid, sulbactam or tazobactam. These inhibitor compete with the β-lactam antibiotics for the active site of the enzyme. The emergence of β-lactamases that possess resistance to the available inactivators necessitate the search for novel inhibitors. In this respect, allosteric binding sites serve as important targets for inhibitor discovery Unlike conventional inhibitiors which target the active site of an enzyme, allosteric inhibitors bind remotely from the active site to regulate protein fucntion. In addition to this, allosteric inhibitors do not compete with the substrate for binding. For these reasons enzyme inhibition via allostery represents a significant challenge to structure-based drug design. Recent structural studies have shown that a number of pockets outside the active site exists in β-lactamase that may serve as viable drug targets.
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