Thiopeps – Thiostrepton derivatives as new antibiotics and specifically designed molecular sensors

An increasing problem in modern medicine is the growing

resistance of microorganisms against antibiotics and the resulting race for new antibiotic candidates. Inventors from the University of Dortmund have found a way to get to both, new antibiotics and a method to identify them. Common thiopeptides like thiostrepton are potent inhibitors of the bacterial protein-biosynthesis. Most prokaryotic ribosomes are known to be thiopeptide sensitive. Mitochondrial ribosomes from protozoa (e.g. Plasmodium, Toxoplasma) and from multicellular organisms (cancer cell lines) are also affected, but not the cytoplasmic ribosomes in eukaryotes. No thiopeptide antibiotic is in human pharmaceutical application so far. The inventions provide novel compounds binding not only to prokaryotic but also to mitochondrial ribosomes. The disclosed compounds are thiostrepton derivatives and inhibit protein biosynthesis. They are stable and show both high affinity and selectivity.

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