Inhibition of “superbugs” molecule inhibitors.

Shanghai Institute of Materia Medica Chinese Academy of Sciences, led an international research group, the calculation of 300,000 kinds of compounds screened discovered a class of compounds capable of inhibiting triazolothiadiazole GGT.

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An international research group led by Shanghai Institute of Materia Medica Chinese Academy of Sciences, the calculation of 300,000 kinds of compounds screened discovered a class of compounds capable of inhibiting triazolothiadiazole GGT, which is a Staphylococcus aureus cell surface protein involved in pathogenicity , and may prevent the emergence of Staphylococcus aureus in mice infected blood, suggesting that this compound may have potential as a response to a treatment of methicillin-resistant Staphylococcus aureus. Related Articles published in “PNAS” magazine September 2, 2014 in.

China, the United States and French scientists on the 1st report that in the United States, “National Academy of Sciences”, the kind of small-molecule inhibitors inhibit methicillin-resistant Staphylococcus aureus infections, with the potential to be to deal with this “superbug” new therapies .

Head of Research, Shanghai Institute of Materia Medica, Chinese Academy of Young Choi also said that multi-drug resistant nosocomial infection has become a global public health threat, which is the most common bacteria methicillin-resistant Staphylococcus aureus.The traditional antibiotic therapy faces two major problems: First, the increasingly serious problem of drug resistance; Second increasingly prominent side effects, such as the host does not lead to metabolic disorders reversibly, and therefore the urgent need to find new therapies.

Choi Yang Guang Luo drugs with Shanghai Fudan University and the University of researchers and institutions, such as Chicago counterparts, through the calculation of 300,000 kinds of compounds discovered a compound screening, medicinal chemistry synthesis method for re-use of improved its activity. The results show that, SrtA obtained small molecule inhibitors inhibit S. aureus infection.

Further animal experiments confirmed that this small molecule inhibitors, although not sterilization, nor inhibit the growth of bacteria, but can reduce the virulence of S. aureus, thereby significantly prolong the survival of infected mice.

Choi Yang Guang to Xinhua News Agency, told reporters: “This is not sterilization but effective inhibitors inhibit bacterial infection, can be used as a preventive strategy to reduce the risk of nosocomial infection in high-risk patients, such as in combination with traditional antibiotics, it is possible to reduce the dose of traditional clinical use of antibiotics. and prolong the life of the clinical medicine. ”

Young Choi Kwong said, SrtA small molecule inhibitors may also prophylactic treatment of other Gram-positive bacteria infections, such as Bacillus anthracis, and Streptococcus pneumoniae. But he also cautioned that further work is needed to verify whether such small molecule inhibitors will produce different from the traditional mechanisms of antibiotic resistance, and whether it also has side effects, such as traditional antibiotics like intestinal flora.

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