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Inhibitors of staphylococcus SarA protein function involved in the expression of staphylococcal virulence factors and the use thereof in treating staphylococcal infections
Inhibitors of staphylococcus SarA protein function involved in the expression of staphylococcal virulence factors and the use thereof in treating staphylococcal infections
The present invention relates to inhibitors of iStaphylococcus/i SarA protein function involved in the expression of staphylococcal virulence factors and the use of these inhibitors to treat and prevent staphylococcal infections in subjects. Particularly, the inhibitors act to interfere with the binding of the SarA protein to its binding site(s). The selection of specific inhibitors of the SarA protein is made possible as a result of the identification of the binding sites of SarA protein on at least a portion of the iagr/i (accessory gene regulator) gene, a gene that like the isar/i (staphylococcal accessory regulator) gene, plays a role in the virulence of iStaphylococcus/i. The present invention also is directed to a method of designing, synthesizing and identifying inhibitors of SarA function and its role in the expression of staphylococcal virulence factors.
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机译:本发明涉及参与葡萄球菌毒力因子表达的葡萄球菌SarA蛋白功能抑制剂,以及这些抑制剂在治疗和预防受试者葡萄球菌感染中的用途。特别地,抑制剂起到干扰SarA蛋白与其结合位点的结合的作用。通过鉴定至少在部分 agr i>(辅助基因调节剂)基因上的SarA蛋白结合位点,可以选择SarA蛋白的特异性抑制剂。像 sar i>(葡萄球菌辅助调节剂)基因一样,在葡萄球菌 i>的毒力中起作用。本发明还涉及设计,合成和鉴定SarA功能抑制剂及其在葡萄球菌毒力因子表达中的作用的方法。
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