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    • 3. 发明申请
    • A HIGH THROUGHPUT PROTEIN INTERACTION ASSAY
    • 高通量蛋白质相互作用测定
    • WO2009117409A2
    • 2009-09-24
    • PCT/US2009/037390
    • 2009-03-17
    • MERCK & CO., INC.CAULFIELD, Michael, J.MILLER, Michael, D.JOYCE, JosephZUCK, Paul, D.GETTY, Krista, L.DUDKIN, VadimOTTINGER, Elizabeth, A.
    • CAULFIELD, Michael, J.MILLER, Michael, D.JOYCE, JosephZUCK, Paul, D.GETTY, Krista, L.DUDKIN, VadimOTTINGER, Elizabeth, A.
    • C12Q1/70
    • G01N33/564C07D211/60C07D211/62C07D401/12C12Q1/18G01N2333/162G01N2333/18G01N2333/22G01N2500/02
    • The present invention relates to a method to identify small molecules that can be used as therapeutics and/or vaccines to prevent, alleviate or ameliorate a pathogenic infection or an autoimmune disorder. The assay of the invention can be used to screen small molecule test compounds for the ability to disrupt particular antigen-antibody interactions of interest. In one embodiment, the antigen is a pathogen-derived antigen and the antibody decreases or inhibits virulence of the pathogen when bound to the antigen (e.g., a neutralizing antibody, antibody with serum bactericidal activity, etc.). Compounds that bind to the antibody to inhibit its binding to antigen can be used as immunogens to elicit production of endogenously produced antibodies having the ability to decrease or inhibit virulence of the pathogen. Compounds that bind to the antigen to inhibit antibody binding can be used as therapeutics to decrease or inhibit pathogen virulence. In another embodiment, the antigen is a self-antigen (autoantigen) and the antibody is an autoantibody that is known to be associated with a pathological condition (e.g., autoimmune disorder). Compounds that bind to the antigen or antibody disrupt binding can be used as therapeutics to decrease or inhibit the autoimmune disorder.
    • 本发明涉及鉴定可用作治疗剂和/或疫苗以预防,缓解或改善病原性感染或自身免疫性疾病的小分子的方法。 本发明的测定可用于筛选小分子测试化合物以破坏感兴趣的特定抗原 - 抗体相互作用的能力。 在一个实施方案中,抗原是病原体衍生的抗原,当与抗原结合时,抗体降低或抑制病原体的毒力(例如,中和抗体,具有血清杀菌活性的抗体等)。 结合抗体以抑制其与抗原结合的化合物可用作免疫原,以引起具有降低或抑制病原体毒性能力的内源性产生抗体的产生。 与抗原结合以抑制抗体结合的化合物可用作降低或抑制病原体毒力的治疗剂。 在另一个实施方案中,抗原是自身抗原(自身抗原),抗体是已知与病理状况(例如自身免疫性疾病)相关的自身抗体。 与抗原或抗体结合的化合物破坏结合可用作治疗剂以减少或抑制自身免疫性疾病。