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    Stat3 inhibitor having anti-cancer activity and methods
    3.
    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
    4.
    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。

    Peptidomimetic inhibitors of STAT activity and uses thereof
    8.
    发明申请
    Peptidomimetic inhibitors of STAT activity and uses thereof 有权
    STAT活性的拟肽抑制剂及其用途

    公开(公告)号：US20050004009A1

    公开(公告)日：2005-01-06

    申请号：US10784309

    申请日：2004-02-20

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

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

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61P35/00 ,  C07K5/04 ,  C07K5/06 ,  C07K5/08 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/06191 ,  C07K5/0827

    摘要： The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are peptidomimetics that inhibit STAT function. Peptidomimetics of the invention include compounds of the formula RY*L (where Y* represents phosphotyrosine), with the R group at the Y-1 position. Peptidomimetics of the invention disrupt Stat3 activation and function. Peptidomimetics of the invention significantly inhibit tumor cell growth and induce tumor cell death.

    摘要翻译： 本发明涉及用于阻断癌细胞生长或增殖和/或诱导癌细胞死亡的组合物和方法。 本发明的组合物是抑制STAT功能的肽模拟物。 本发明的肽模拟物包括式RY * L（其中Y *表示磷酸酪氨酸）的化合物，其中R基团在Y-1位。 本发明的肽模拟物破坏Stat3的活化和功能。 本发明的肽模拟物显着抑制肿瘤细胞生长并诱导肿瘤细胞死亡。

    Growth Factor Binding Molecules
    9.
    发明申请
    Growth Factor Binding Molecules 有权
    生长因子结合分子

    公开(公告)号：US20100210516A1

    公开(公告)日：2010-08-19

    申请号：US12622295

    申请日：2009-11-19

    申请人： Said Sebti ,  Andrew D. Hamilton

    发明人： Said Sebti ,  Andrew D. Hamilton

    IPC分类号： A61K38/12 ,  C07K7/56 ,  A61P9/10 ,  A61P9/00

    CPC分类号： C07K7/56 ,  A61K38/00 ,  C07K14/001

    摘要： Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.

    摘要翻译： 生长因子结合分子，其具有连接到非肽有机支架上的多个肽环，优选具有具有四个氨基酸侧链的假六个氨基酸肽环。 生长因子结合分子特异性结合各种生长因子并且适用于治疗具有肿瘤或再狭窄的受试者。 在一个实施方案中，公开了用于抑制实体瘤中肿瘤生长和血管生成的血小板衍生生长因子结合分子。

    Growth factor binding molecules
    10.
    发明授权
    Growth factor binding molecules 有权
    生长因子结合分子

    公开(公告)号：US07157419B2

    公开(公告)日：2007-01-02

    申请号：US09811945

    申请日：2001-03-21

    申请人： Said Sebti ,  Andrew D. Hamilton

    发明人： Said Sebti ,  Andrew D. Hamilton

    IPC分类号： C07K5/10 ,  C07K6/50

    CPC分类号： C07K7/56 ,  A61K38/00 ,  C07K14/001

    摘要： Growth factor binding molecules having a plurality of peptide loops attached to a non-peptide organic scaffold, preferably having pseudo-six amino acid peptide loops with four amino acid sidechains. The growth factor binding molecules specifically bind various growth factors and are suitable for treating a subject having tumors or restinosis. In one embodiment a platelet-derived growth factor binding molecule is disclosed that is used to inhibit tumor growth and angiogenesis in solid tumors.

    摘要翻译： 生长因子结合分子，其具有连接到非肽有机支架上的多个肽环，优选具有具有四个氨基酸侧链的假六个氨基酸肽环。 生长因子结合分子特异性结合各种生长因子并且适用于治疗具有肿瘤或再狭窄的受试者。 在一个实施方案中，公开了用于抑制实体瘤中肿瘤生长和血管生成的血小板衍生生长因子结合分子。