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1. 发明申请

US20100285026A1 PHOSPHORYLATION OF HISTONE H3 AT THREONINE 11 - A NOVEL EPIGENETIC MARK FOR TRANSCRIPTIONAL REGULATION 失效
标题翻译： HISTONE H3在THREONINE 11的磷酸化 - 一个新的重要标志进行转录调节
公开(公告)号：US20100285026A1
公开(公告)日：2010-11-11
申请号：US12669294
申请日：2008-05-27
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： A61K39/395 , C12N5/02 , C12Q1/48 , A61P35/00
CPC分类号： C07K14/47 , A61K38/00 , C07K14/721 , C07K16/40 , C12N9/1205 , C12N15/1137 , C12N2310/111 , C12N2310/14 , C12Q1/485 , C12Y207/11013 , G01N33/57434 , G01N2333/723 , G01N2333/91215 , G01N2500/00
摘要： The present invention relates to a process for controlling at least one androgen receptor- (AR-) regulated mechanism in mammalian cells under histone-phosphorylating conditions, said process comprising allowing at least one inhibitor with specificity for at least one protein kinase C-related kinase (PRK) to act on said at least one PRK1 thereby modulating, preferably down-regulating, the activity of said at least one PRK and optionally blocking said at least one androgen receptor-regulated mechanism in said mammalian cells.
摘要翻译：本发明涉及在组蛋白 - 磷酸化条件下控制哺乳动物细胞中至少一种雄激素受体（AR））调节机制的方法，所述方法包括允许至少一种具有至少一种蛋白激酶C相关激酶特异性的抑制剂（PRK）作用于所述至少一种PRK1，从而调节，优选下调所述至少一种PRK的活性，并任选地阻断所述哺乳动物细胞中的所述至少一种雄激素受体调节机制。

2. 发明授权

US08680157B2 Androgen receptor-dependent gene expression control 有权
标题翻译：雄激素受体依赖基因表达控制
公开(公告)号：US08680157B2
公开(公告)日：2014-03-25
申请号：US11884568
申请日：2006-02-16
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： A61P13/08
CPC分类号： A61K31/138 , A61K31/137 , A61K31/7088 , C12Q1/26 , C12Q1/48 , G01N33/743 , G01N2333/91011 , G01N2500/04
摘要： The invention relates to the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to assay systems allowing to test LSD1 inhibitors for their ability to inhibit LSD1 function.
摘要翻译：本发明涉及至少一种胺氧化酶抑制剂用于调节哺乳动物中赖氨酸特异性脱甲基酶（LSD1）的活性和用于控制雄激素受体依赖性基因表达的药物组合物的用途，其包含至少有效剂量一种适于调节哺乳动物赖氨酸特异性脱甲基酶（LSD1）活性的胺氧化酶抑制剂。本发明还涉及允许测试LSD1抑制剂抑制LSD1功能的能力的测定系统。

3. 发明授权

US07767411B2 Assay system for specific inhibitors of protein kinase C-related kinases 失效
标题翻译：蛋白激酶C相关激酶特异性抑制剂的测定系统
公开(公告)号：US07767411B2
公开(公告)日：2010-08-03
申请号：US10592313
申请日：2005-03-10
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： C12Q1/48
CPC分类号： G01N33/5011 , G01N33/566 , G01N2333/9121
摘要： The present invention relates to an assay system for specific inhibitors of protein kinase C-related kinases (PRKs) relating to one or more of the reactions wherein said protein kinase C-related kinases are involved under physiological conditions. The invention also relates to a process for identifying specific inhibitors for protein kinase C-related kinases.
摘要翻译：本发明涉及与一种或多种反应相关的蛋白激酶C-相关激酶（PRK）的特异性抑制剂的测定系统，其中所述蛋白激酶C-相关激酶参与生理条件。本发明还涉及用于鉴定蛋白激酶C相关激酶的特异性抑制剂的方法。

4. 发明授权

US09370499B2 Androgen receptor-dependent gene expression control 有权
标题翻译：雄激素受体依赖基因表达控制
公开(公告)号：US09370499B2
公开(公告)日：2016-06-21
申请号：US14172515
申请日：2014-02-04
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： A61K31/138 , A61K31/137 , A61K31/7088 , C12Q1/26 , C12Q1/48 , G01N33/74
CPC分类号： A61K31/138 , A61K31/137 , A61K31/7088 , C12Q1/26 , C12Q1/48 , G01N33/743 , G01N2333/91011 , G01N2500/04
摘要： Disclosed is the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal.
摘要翻译：公开了至少一种胺氧化酶抑制剂用于调节哺乳动物中赖氨酸特异性脱甲基酶（LSD1）的活性和用于控制雄激素受体依赖性基因表达的药物组合物的用途，其包含有效剂量的至少一种胺适用于调节哺乳动物赖氨酸特异性脱甲基酶（LSD1）的活性的氧化酶抑制剂。

5. 发明授权

US08076094B2 Phosphorylation of histone H3 at threonine 11—a novel epigenetic mark for transcriptional regulation 失效
标题翻译：苏氨酸11组蛋白H3的磷酸化 - 转录调控的新表观遗传标记
公开(公告)号：US08076094B2
公开(公告)日：2011-12-13
申请号：US12669294
申请日：2008-05-27
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： G01N33/574 , G01N33/53
CPC分类号： C07K14/47 , A61K38/00 , C07K14/721 , C07K16/40 , C12N9/1205 , C12N15/1137 , C12N2310/111 , C12N2310/14 , C12Q1/485 , C12Y207/11013 , G01N33/57434 , G01N2333/723 , G01N2333/91215 , G01N2500/00
摘要： The present invention relates to a process for controlling at least one androgen receptor- (AR-) regulated mechanism in mammalian cells under histone-phosphorylating conditions, said process comprising allowing at least one inhibitor with specificity for at least one protein kinase C-related kinase (PRK) to act on said at least one PRK1 thereby modulating, preferably down-regulating, the activity of said at least one PRK and optionally blocking said at least one androgen receptor-regulated mechanism in said mammalian cells.
摘要翻译：本发明涉及在组蛋白 - 磷酸化条件下控制哺乳动物细胞中至少一种雄激素受体（AR））调节机制的方法，所述方法包括允许至少一种具有至少一种蛋白激酶C相关激酶特异性的抑制剂（PRK）作用于所述至少一种PRK1，从而调节，优选下调所述至少一种PRK的活性，并任选地阻断所述哺乳动物细胞中的所述至少一种雄激素受体调节机制。

6. 发明申请

US20120096568A1 TRANSGENIC LSD1 ANIMAL MODEL FOR CANCER 审中-公开
标题翻译： TRANSGENIC LSD1动物模型
公开(公告)号：US20120096568A1
公开(公告)日：2012-04-19
申请号：US13376212
申请日：2010-04-28
申请人： Roland Schuele , Thomas Guenther , Eric Metzger
发明人： Roland Schuele , Thomas Guenther , Eric Metzger
IPC分类号： A61K49/00 , C12N15/85 , A01K67/027
CPC分类号： C12N15/8509 , A01K2217/072 , A01K2227/105 , A01K2267/0331
摘要： The present invention relates to a non-human transgenic animal whose genome comprises a stably integrated transgenic nucleotide sequence encoding Lysine-specific Demethylase 1 (LSD1) operably linked to a promoter. The invention further concerns methods for generating the non-human animal and its use as a cancer model.
摘要翻译：本发明涉及非人转基因动物，其基因组包含可操作地连接于启动子的编码赖氨酸特异性脱甲基酶1（LSD1）的稳定整合的转基因核苷酸序列。本发明还涉及产生非人类动物的方法及其作为癌症模型的用途。

7. 发明申请

US20080139665A1 Androgen Receptor-Dependent Gene Expression Control 有权
标题翻译：雄激素受体依赖基因表达控制
公开(公告)号：US20080139665A1
公开(公告)日：2008-06-12
申请号：US11884568
申请日：2006-02-16
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： A61K31/137 , C12Q1/48
CPC分类号： A61K31/138 , A61K31/137 , A61K31/7088 , C12Q1/26 , C12Q1/48 , G01N33/743 , G01N2333/91011 , G01N2500/04
摘要： The invention relates to the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to assay systems allowing to test LSD1 inhibitors for their ability to inhibit LSD1 function.
摘要翻译：本发明涉及至少一种胺氧化酶抑制剂用于调节哺乳动物中赖氨酸特异性脱甲基酶（LSD1）的活性和用于控制雄激素受体依赖性基因表达的药物组合物的用途，其包含至少有效剂量一种适于调节哺乳动物赖氨酸特异性脱甲基酶（LSD1）活性的胺氧化酶抑制剂。本发明还涉及允许测试LSD1抑制剂抑制LSD1功能的能力的测定系统。

8. 发明申请

US20070196882A1 Assay system for specific inhibitors of protein kinase c-related kinases 失效
标题翻译：蛋白激酶c相关激酶特异性抑制剂的测定系统
公开(公告)号：US20070196882A1
公开(公告)日：2007-08-23
申请号：US10592313
申请日：2005-03-10
申请人： Roland Schuele , Eric Metzger
发明人： Roland Schuele , Eric Metzger
IPC分类号： C12Q1/48 , A61K31/56
CPC分类号： G01N33/5011 , G01N33/566 , G01N2333/9121
摘要： The present invention relates to an assay system for specific inhibitors of protein kinase C-related kinases (PRKs) relating to one or more of the reactions wherein said protein kinase C-related kinases are involved under physiological conditions. The invention also relates to a process for identifying specific inhibitors for protein kinase C-related kinases.
摘要翻译：本发明涉及与一种或多种反应相关的蛋白激酶C-相关激酶（PRK）的特异性抑制剂的测定系统，其中所述蛋白激酶C-相关激酶参与生理条件。本发明还涉及用于鉴定蛋白激酶C相关激酶的特异性抑制剂的方法。

9. 发明申请

US20070031395A1 Repressor of skeletal muscle differentiation, nucleic acid coding therefor and the use thereof in diagnosis and therapy 审中-公开
标题翻译：骨骼肌分化抑制剂，其编码的核酸及其在诊断和治疗中的用途
公开(公告)号：US20070031395A1
公开(公告)日：2007-02-08
申请号：US10507780
申请日：2003-03-13
申请人： Roland Schuele , Philip Hublitz
发明人： Roland Schuele , Philip Hublitz
IPC分类号： A61K38/54 , C07H21/04 , C12P21/06 , C12N9/99 , C12N15/86
CPC分类号： C07K16/18 , A61K38/00 , C07K14/4703 , C07K14/4716
摘要： Polypeptide sequences which play a part in the regulation of skeletal muscle differentiation, and nucleic acids coding therefor, and the use thereof in diagnosis and therapy are disclosed. Possible uses are also indicated for antibodies which are directed against corresponding epitopes of the GRIM1 polypeptide.
摘要翻译：公开了在骨骼肌分化调节中起作用的多肽序列及其编码的核酸及其在诊断和治疗中的应用。对于针对GRIM1多肽的相应表位的抗体也可以使用可能的用途。

10. 发明申请

US20090104196A1 Antibodies For Use in Identifying and/or Scoring Prostate Cancer and Androgen Receptor-Dependent Gene Expression Control 有权
标题翻译：用于鉴定和/或评估前列腺癌和雄激素受体依赖基因表达控制的抗体
公开(公告)号：US20090104196A1
公开(公告)日：2009-04-23
申请号：US11995387
申请日：2006-07-13
申请人： Roland Schuele , Erich Metzger , Reinhard Buettner
发明人： Roland Schuele , Erich Metzger , Reinhard Buettner
IPC分类号： A61K39/395 , C07K16/18 , G01N33/574 , C07H21/00 , A61K31/70 , A61P43/00
CPC分类号： G01N33/57434 , C07K16/3069 , C07K16/40 , G01N33/573 , G01N33/743 , G01N2500/00
摘要： The invention relates to antibodies for use for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical and diagnostical compositions comprising such antibodies. The invention also relates to a method for identifying and/or scoring prostate carcinomas. Furthermore, the invention relates to the use of at least one siRNA (“short interfering RNA”) and/or at least one anti-LSD1 antibody for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal or for the manufacture of a medicament for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to a pharmaceutical composition for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one siRNA and/or at least one anti-LSD1 antibody suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to a method for controlling the androgen receptor-dependent gene expression in a mammal, said process comprising the step of administering to said mammal, on a suitable route, an effective dose of a pharmaceutical composition modulating an activity of the lysine-specific demethylase (LSD1) in a mammal.
摘要翻译：本发明涉及用于调节哺乳动物中赖氨酸特异性脱甲基酶（LSD1）的活性的抗体以及包含此类抗体的药物和诊断组合物。本发明还涉及用于鉴定和/或评分前列腺癌的方法。此外，本发明涉及至少一种siRNA（“短干扰RNA”）和/或至少一种抗LSD1抗体用于调节哺乳动物或制造中的赖氨酸特异性脱甲基酶（LSD1）的活性的用途的用于调节哺乳动物中赖氨酸特异性脱甲基酶（LSD1）的活性的药物。本发明还涉及用于控制雄激素受体依赖性基因表达的药物组合物，其包含有效剂量的至少一种siRNA和/或至少一种抗LSD1抗体，其适于调节赖氨酸特异性脱甲基酶（LSD1 ）在哺乳动物中。本发明还涉及一种用于控制哺乳动物中雄激素受体依赖性基因表达的方法，所述方法包括以下步骤：在合适的途径向所述哺乳动物施用有效剂量的调节赖氨酸 - 特异性脱甲基酶（LSD1）。

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