Newly Modified Vancomycin Has Three Independent Mechanisms of Action & Is 1,000-Fold As Active As Native Vancomycin

Scientists at The Scripps Research Institute (TSRI) have given new superpowers to a lifesaving antibiotic called vancomycin, an advance that could eliminate the threat of antibiotic-resistant infections for years to come. The researchers, led by Dale Boger, PhD, Co-Chair of TSRI's Department of Chemistry, discovered a way to structurally modify vancomycin to make an already-powerful version of the antibiotic even more potent. "Doctors could use this modified form of vancomycin without fear of resistance emerging," said Dr. Boger, whose team announced the finding that was published online on May 30, 2017 in PNAS. The article is titled “Peripheral Modifications of [Ψ[CH2NH]Tpg4]Vancomycin with Added Synergistic Mechanisms of Action Provide Durable and Potent Antibiotics.” The original form of vancomycin is an ideal starting place for developing better antibiotics. The antibiotic has been prescribed by doctors for 60 years, and bacteria are only now developing resistance to it. This suggests bacteria already have a hard time overcoming vancomycin's original "mechanism of action," which works by disrupting how bacteria form cell walls. Dr. Boger called vancomycin "magical" for its proven strength against infections, and previous studies by Boger and his colleagues at TSRI had shown that it is possible to add two modifications to vancomycin to make it even more potent. "With these modifications, you need less of the drug to have the same effect," Dr. Boger said.
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