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29 条记录 (耗时 0.033 秒)

    INHIBITION OF CELL PROLIFERATION
    21.
    发明申请
    INHIBITION OF CELL PROLIFERATION 有权
    抑制细胞增殖

    公开(公告)号：US20070254318A1

    公开(公告)日：2007-11-01

    申请号：US11562903

    申请日：2006-11-22

    申请人： Said Sebti ,  Srikumar Chellappan ,  Nicholas Lawrence

    发明人： Said Sebti ,  Srikumar Chellappan ,  Nicholas Lawrence

    IPC分类号： A61K31/155 ,  A61K31/215 ,  A61K31/34 ,  A61K31/41 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/675 ,  C07D233/00 ,  C07D249/12 ,  C12N5/08 ,  G01N33/50

    CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

    摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

    摘要翻译： 所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，其中80nM至500nM的IC 50 N值。 此外，这些化合物令人惊奇地有效地抑制多种癌细胞，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和 前列腺癌。 此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。 因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。

    Effective treatment of tumors and cancer with triciribine and related compounds
    22.
    发明申请
    Effective treatment of tumors and cancer with triciribine and related compounds 有权

    公开(公告)号：US20060247188A1

    公开(公告)日：2006-11-02

    申请号：US11096082

    申请日：2005-03-29

    申请人： Jin Cheng ,  Said Sebti

    发明人： Jin Cheng ,  Said Sebti

    IPC分类号： A61K31/7076

    CPC分类号： C07H17/02 ,  A61K31/7064

    摘要： The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat tumors and cancer by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.

    Stat3 inhibitor having anti-cancer activity and methods
    24.
    发明授权
    Stat3 inhibitor having anti-cancer activity and methods 有权
    Stat3抑制剂具有抗癌活性和方法

    公开(公告)号：US08609639B2

    公开(公告)日：2013-12-17

    申请号：US12517453

    申请日：2007-12-05

    申请人： James Turkson ,  Said Sebti ,  Richard Jove ,  Andrew D. Hamilton

    发明人： James Turkson ,  Said Sebti ,  Richard Jove ,  Andrew D. Hamilton

    IPC分类号： A61K31/675 ,  C07F9/653 ,  C12N5/071

    CPC分类号： C07F9/653

    摘要： A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.

    摘要翻译： 描述了一种小分子Stat3二聚体抑制剂S3I-M2001，阐明了Stat3化学探针抑制剂生物化学和生物学效应背景下激活的Stat3的细胞内加工动力学。 S3I-M2001是Stat3 Src同源性（SH）2结构域结合磷酸酪氨酸肽的新鉴定的基于恶唑的拟肽，其选择性地破坏活性Stat3：Stat3二聚体。 S3I-M2001抑制Stat3依赖性恶性转化，存活，迁移和入侵持续激活Stat3的小鼠和人类癌细胞。 S3I-M2001抑制Stat3依赖的转录调控肿瘤生存基因，如Bcl-xL。 所公开的化合物可用作某些癌症的新的潜在治疗。

    Stat3 Inhibitor Having Anti-Cancer Activity and Methods
    25.
    发明申请
    Stat3 Inhibitor Having Anti-Cancer Activity and Methods 有权
    Stat3抑制剂具有抗癌活性和方法

    公开(公告)号：US20110124602A1

    公开(公告)日：2011-05-26

    申请号：US12517453

    申请日：2007-12-05

    申请人： James Turkson ,  Said Sebti ,  Richard Jove ,  Andrew D. Hamilton

    发明人： James Turkson ,  Said Sebti ,  Richard Jove ,  Andrew D. Hamilton

    IPC分类号： A61K31/675 ,  C07F9/653 ,  C12N5/071 ,  C12N5/09 ,  A61P35/00 ,  A61P35/04

    CPC分类号： C07F9/653

    摘要： A small-molecule Stat3 dimerization inhibitor, S3I-M2001, is described and the dynamics of intracellular processing of activated Stat3 within the context of the biochemical and biological effects of the Stat3 chemical probe inhibitor are elucidated. S3I-M2001 is a newly-identified oxazole-based peptidomimetic of the Stat3 Src Homology (SH) 2 domain-binding phosphotyrosine peptide that selectively disrupts active Stat3:Stat3 dimers. Stat3-dependent malignant transformation, survival, and migration and invasion of mouse and human cancer cells harboring persistently-activated Stat3 were inhibited by S3I-M2001. S3I-M2001 inhibited Stat3-dependent transcriptional regulation of tumor survival genes, such as Bcl-xL. The disclosed compound is useful as a new potential treatment for certain cancers.

    摘要翻译： 描述了一种小分子Stat3二聚体抑制剂S3I-M2001，阐明了Stat3化学探针抑制剂生物化学和生物学效应背景下激活的Stat3的细胞内加工动力学。 S3I-M2001是Stat3 Src同源性（SH）2结构域结合磷酸酪氨酸肽的新鉴定的基于恶唑的拟肽，其选择性地破坏活性Stat3：Stat3二聚体。 S3I-M2001抑制Stat3依赖性恶性转化，存活，迁移和入侵持续激活Stat3的小鼠和人类癌细胞。 S3I-M2001抑制Stat3依赖的转录调控肿瘤生存基因，如Bcl-xL。 所公开的化合物可用作某些癌症的新的潜在治疗。

    Inhibition of the Raf/Mek/P-Erk pathway for treating cancer
    27.
    发明申请
    Inhibition of the Raf/Mek/P-Erk pathway for treating cancer 有权
    抑制Raf / Mek / P-Erk途径治疗癌症

    公开(公告)号：US20070021512A1

    公开(公告)日：2007-01-25

    申请号：US11490777

    申请日：2006-07-21

    申请人： Said Sebti

    发明人： Said Sebti

    IPC分类号： A61K31/138

    CPC分类号： A61K31/138 ,  G01N33/574

    摘要： The invention disclosed herein provides for methods of treating cancer using inhibitors of the Raf/Mek/P-Erk 1/2 pathway. These inhibitors include B2AR agonists (such as ARA-211 (pirbuterol) and isoproterenol), adenylyl cyclase activators, cAMP analogs and Epac activators. The invention also provides methods for diagnosing cancer in an individual.

    摘要翻译： 本文公开的本发明提供了使用Raf / Mek / P-Erk 1/2途径的抑制剂治疗癌症的方法。 这些抑制剂包括B2AR激动剂（例如ARA-211（吡布特罗）和异丙肾上腺素），腺苷酸环化酶激活剂，cAMP类似物和Epac激活剂。 本发明还提供了诊断个体癌症的方法。

    RhoB variants and methods of use
    28.
    发明申请
    RhoB variants and methods of use 有权
    RhoB变体和使用方法

    公开(公告)号：US20060105374A1

    公开(公告)日：2006-05-18

    申请号：US11274368

    申请日：2005-11-14

    申请人： Said Sebti

    发明人： Said Sebti

    IPC分类号： C12Q1/68 ,  A61K38/16 ,  C07H21/04 ,  C12P21/06 ,  C12N9/16 ,  C12N15/86

    CPC分类号： C07K14/82 ,  A61K38/00 ,  C12N9/16

    摘要： In one aspect, the present invention concerns RhoB variant polypeptides and isolated degenerate polynucleotides encoding the RhoB variant polypeptides. In another aspect, the present invention concerns nucleic acid constructs containing a polynucleotide encoding a RhoB variant polypeptide, and host cells genetically modified to express such polynucleotides. In another aspect, the present invention provides a method of inhibiting the growth of, and inducing apoptosis in, cancerous cells by contacting the cells with an effective amount of a RhoB variant.

    摘要翻译： 一方面，本发明涉及编码RhoB变体多肽的RhoB变体多肽和分离的简并多核苷酸。 另一方面，本发明涉及含有编码RhoB变体多肽的多核苷酸和经遗传修饰以表达该多核苷酸的宿主细胞的核酸构建体。 另一方面，本发明提供了通过使细胞与有效量的RhoB变体接触来抑制癌细胞的生长和诱导细胞凋亡的方法。