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    • 5. 发明申请
    • COMPOSITIONS AND METHODS FOR MODULATING SIRTUIN ACTIVITY
    • 用于调节SIRTUIN活性的组合物和方法
    • US20100160262A1
    • 2010-06-24
    • US12343177
    • 2008-12-23
    • Melanie OttEric M. VerdinManfred Jung
    • Melanie OttEric M. VerdinManfred Jung
    • A61K31/655G01N33/573A61K31/538A61K31/551A61K31/497A61K31/506A61K31/52A61K31/4725
    • A61K31/4725A61K31/497A61K31/506A61K31/52A61K31/538A61K31/551A61K31/655
    • The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide. The present invention further provides active agents that modulate sirtuin activity or expression; and compositions, including pharmaceutical compositions, comprising the active agents.
    • 本发明提供了涉及调节沉默调节蛋白的活性和/或sirtuin mRNA和/或sirtuin多肽水平的治疗方法。 在一些实施方案中,本发明提供了涉及调节SIRT1活性和/或SIRT mRNA和/或多肽水平的治疗方法。 本发明提供抑制SIRT1 Tat脱乙酰酶活性的方法。 抑制SIRT1 Tat脱乙酰酶活性的方法可用于治疗免疫缺陷病毒感染,特别是人类免疫缺陷病毒(HIV)感染。 因此,本发明提供了治疗免疫缺陷病毒感染的方法,通常涉及抑制SIRT1 Tat脱乙酰酶的活性。 本发明进一步提供了鉴定调节沉默调节蛋白的活性(例如,SIRT1活性)的药剂的方法,特别是sirtuins与底物(例如,结合和/或脱乙酰化)例如病毒底物如Tat多肽的能力。 本发明还提供调节沉默调节蛋白的活性或表达的活性剂; 和包含活性剂的组合物,包括药物组合物。
    • 9. 发明授权
    • Screening methods for the identification of agents that inhibit SIRT1 Tat deacetylase activity
    • 用于鉴定抑制SIRT1 Tat脱乙酰酶活性的试剂的筛选方法
    • US07485416B2
    • 2009-02-03
    • US11022192
    • 2004-12-22
    • Melanie OttEric M. VerdinManfred Jung
    • Melanie OttEric M. VerdinManfred Jung
    • C12Q1/70A61K39/21
    • C12Q1/34C12Q1/26G01N2333/16G01N2333/918G01N2333/98G01N2500/02
    • The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide. The present invention further provides active agents that modulate sirtuin activity or expression; and compositions, including pharmaceutical compositions, comprising the active agents.
    • 本发明提供了涉及调节沉默调节蛋白的活性和/或sirtuin mRNA和/或sirtuin多肽水平的治疗方法。 在一些实施方案中,本发明提供了涉及调节SIRT1活性和/或SIRT mRNA和/或多肽水平的治疗方法。 本发明提供抑制SIRT1 Tat脱乙酰酶活性的方法。 抑制SIRT1 Tat脱乙酰酶活性的方法可用于治疗免疫缺陷病毒感染,特别是人类免疫缺陷病毒(HIV)感染。 因此,本发明提供了治疗免疫缺陷病毒感染的方法,通常涉及抑制SIRT1 Tat脱乙酰酶的活性。 本发明进一步提供了鉴定调节沉默调节蛋白的活性(例如,SIRT1活性)的药剂的方法,特别是sirtuins与底物(例如,结合和/或脱乙酰化)例如病毒底物如Tat多肽的能力。 本发明还提供调节沉默调节蛋白的活性或表达的活性剂; 和包含活性剂的组合物,包括药物组合物。