J. Wang et al., "Platensimycin is a selective FabF inhibitor with potent antibiotic properties," Nature, 441:358-61, 2006. (Cited in 91 papers)
Sifting through South African soil samples, scientists at Merck Research Laboratories found a new compound called platensimycin. It is effective against methicillin-resistant Staphylococcus aureus and other multiple-drug-resistant bacteria, thus representing an entirely new class of antibiotic. The researchers used X-ray crystallography and direct-binding assays to show that platensimycin kills bacteria by binding to a key intermediate, called FabF, in enzyme-mediated lipid construction, thus short-circuiting bacterial fatty acid synthesis.
Eric Brown, a biochemist at McMaster University in Canada, hails the Merck team's multidisciplinary approach to revealing platensimycin's mode of action. "It's very difficult, for example, to show that a small molecule would have an affinity for an intermediate in an enzyme-driven reaction," he says.
"This new antibiotic gave us a hope that we've found something that these bacteria cannot defend ...
