Abstract
Researchers have created a modified form of the approved antibacterial drug vancomycin (Vancocin) that has three independent mechanisms of action, boosting its potency and minimizing the potential for bacteria to develop resistance to it. Vancomycin, a bacterial natural product, had long been an antibiotic of last resort because it remained effective against drug-resistant bacteria after other medications stopped working. But bacteria have now evolved defenses against vancomycin, which works by inhibiting transpeptidase, an enzyme that catalyzes a cross-linking reaction bacteria use to build cell walls. Scientists have recently modified vancomycin in various ways to boost its potency and discourage resistance. In fact, the U.S. Food & Drug Administration recently approved three modified vancomycins: oritavancin, dalbavancin, and telavancin. They are each made by semisynthesis from vancomycin by chemical addition or modification of one or two chemical groups. Dale L. Boger of Scripps Research Institute and coworkers have now created what could
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