Antineoplastic activities of ellipticine and its derivatives
    1.
    发明申请
    Antineoplastic activities of ellipticine and its derivatives 审中-公开
    玫瑰树碱及其衍生物的抗肿瘤活性

    公开(公告)号:US20070027175A1

    公开(公告)日:2007-02-01

    申请号:US11494335

    申请日:2006-07-27

    IPC分类号: A61K31/4745

    摘要: The present invention describes selective cell growth inhibition of myeloma cells by ellipticine derivatives, 9-methoxy ellipticine and 9-dimethyl amino-ethoxy ellipticine. The cell growth inhibition efficacy was highest for 9-dimethyl amino-ethoxy ellipticine among the ellipcitine derivatives tested. The cell toxicity of 9-dimethyl amino-ethoxy ellipticine was selective for myeloma cells and did not kill normal cells in the effective antineoplastic dose range. 9-dimethyl amino-ethoxy ellipticine was superior to existing antimyeloma drugs, Adriamycin® and Etoposide in eliciting early and better cell growth inhibition response.

    摘要翻译: 本发明描述了通过玫瑰树碱衍生物,9-甲氧基玫瑰树碱和9-二甲基氨基 - 乙氧基玫瑰树碱对骨髓瘤细胞的选择性细胞生长抑制。 在测试的椭球形衍生物中,9-二甲基氨基乙氧基玫瑰树碱对细胞生长抑制效果最高。 9-二甲基氨基乙氧基玫瑰树碱的细胞毒性对骨髓瘤细胞是选择性的,并且在有效的抗肿瘤剂量范围内不能杀死正常细胞。 9-二甲基氨基乙氧基玫瑰树碱优于现有的抗炎药物,阿霉素和依托泊苷引发早期和更好的细胞生长抑制反应。

    Copy Number Variant-Dependent Genes As Diagnostic Tools, Predictive Biomarkers And Therapeutic Targets
    2.
    发明申请
    Copy Number Variant-Dependent Genes As Diagnostic Tools, Predictive Biomarkers And Therapeutic Targets 审中-公开
    作为诊断工具,预测生物标志物和治疗靶标的拷贝数变异依赖基因

    公开(公告)号:US20130209446A1

    公开(公告)日:2013-08-15

    申请号:US13810705

    申请日:2011-07-20

    摘要: Provided herein are methods of diagnosing and/or treating malignant or pre-malignant conditions in a subject. Overexpression of copy number variant-dependent genes, e.g., genes encoding a cell surface receptor, resulting from copy number changes compared to control is diagnostic of the condition, such as multiple myeloma or monoclonal gammopathy of undetermined significance. Also provided are methods for treating malignant conditions, such as multiple myeloma or a hyperdiploid subtype, with therapeutic agents, with or without other anti-cancer drugs, to downrregulate the overexpressed CNV genes and/or up-regulate the underexpressed genes. Furthermore, methods for lowering drug resistance in multiple myeloma cells via inhibition of platelet activation or thrombin release and for increasing survivability of a multiple myeloma subject via lithibition of PSMD4 gene to increase b-catenin protein expression are provided.

    摘要翻译: 本文提供了诊断和/或治疗受试者中恶性或恶性前病症的方法。 拷贝数变异依赖性基因的过度表达,例如编码细胞表面受体的基因,与对照相比拷贝数变化所得到的是病症的诊断,例如具有未确定意义的多发性骨髓瘤或单克隆丙种球蛋白病。 还提供了用治疗剂(含或不含其他抗癌药物)治疗恶性病症如多发性骨髓瘤或高倍体二倍体亚型的方法来下调调节过表达的CNV基因和/或上调低表达基因。 此外,提供了通过抑制血小板活化或凝血酶释放降低多发性骨髓瘤细胞耐药性的方法,以及通过PSMD4基因通过增加b-连环蛋白表达增加多发性骨髓瘤受试者的生存性。