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May 19, 2008
 |  BioCentury  |  Emerging Company Profile

Cempra: Binding bacteria better

Using a set of in-licensed macrolide chemistry technologies, Cempra Pharmaceuticals Inc. is developing a pipeline of macrolide antibiotics that it hopes will be effective against resistant bacteria but have safety profiles similar to marketed macrolides. The company began Phase I studies of CEM-101 in healthy volunteers this month.

Macrolides inhibit bacterial protein synthesis by binding reversibly to a peptide tunnel on the 50S subunit of the bacterial ribosome, thereby inhibiting translocation of peptidyl-tRNA. This action is mainly bacteriostatic, but can also be bactericidal at high drug concentrations.

The primary mechanism of acquired bacterial resistance to macrolides is post-transcriptional methylation of the 23S bacterial ribosome, which is part of the 50S subunit.

"The technology that we have licensed allows us to create a tighter binding antibiotic - a more effective obstruction. The region of...

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