James Fraser @fraserlab.com · Feb 3 Streptogramins are promising antibiotics for treating resistant bacterial infections, but their efficacy is threatened by Vat enzymes, which inactivate streptogramins by acetylation (blocking a key interaction with the ribosome). So we set out to block the blocker!
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Using X-ray crystallography-based fragment screening, we mapped VatD’s key binding sites and identified small-molecule fragments that can serve as leads. This builds on our 2020 Seiple collaboration, where we modified streptogramins to overcome resistance. www.ncbi.nlm.nih.gov/pmc/articles...