Engineering an Allosteric Binding Site for Aminoglycosides into TEM1-β-Lactamase (pages 904–913)
Dr. Alexander N. Volkov, Dr. Humberto Barrios, Dr. Pascale Mathonet, Dr. Christine Evrard, Prof. Marcellus Ubbink, Prof. Jean-Paul Declercq, Prof. Patrice Soumillion and Prof. Jacques Fastrez
Article first published online: 18 MAR 2011 | DOI: 10.1002/cbic.201000568
Evolving regulation: An allosteric binding site for aminoglycoside antibiotics has been created in TEM1-β-lactamase by directed evolution. Aminoglycosides binding activates the enzyme by expulsion of an inhibitor, and allows their detection at low concentration. Interactions with several ligands offer opportunities for complex allosteric regulation.