Date: 13/09/2018
Authors: Carmen Barambio, Miguel Alonso, Mary Flor Alberca and Carmen Aznar
Superbugs have developed resistance against antibiotics during the past few years, thus the difficulty to fight them has increased. Human beings should stop this problem, because a huge number of deaths are caused by epidemies each year. One of the most importante microorganisms responsible for the problem are gram-negative bacteria; these bacteria have an outer membrane which blocks the activity target of different classes of antibiotics used. Despite extensive efforts no antibiotic has been effective.
A study group led by Christopher Heise from the university of Virginia,has improved the compound called Arylomycins. This compound, is a class of polypeptide which attacks the signal peptidase, an essential membrane-bound enzyme that breaks down proteins and peptides. In gram-negative bacteria, this enzyme is located between the cytoplasmic and the outer membranes. This site was thought to be inaccessible to the arylomycins.
The optimization of arylomycins into a chemical compound with a potent broad-spectrum activity against multi-drug resistante gram-negative bacteria (such as E. coli) has taken place in the last five years. in their mouse-model experiments, they found an arylomycin derivative called G0775, which uses an atypical mechanism to penetrate in the outer membrane that bacteria cannot resist.
Smith, P.A., et al. (2018). Optimized arylomycins are a new class of Gram-negative antibiotics. Nature561:189–194.
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