公开(公告)号：WO2013109388A3

公开(公告)日：2015-02-05

申请号：PCT/US2012071434

申请日：2012-12-21

Applicant: ONCOTHERAPY SCIENCE INC

Inventor： MATSUO YO ,  HISADA SHOJI ,  NAKAMURA YUSUKE ,  AHMED FERYAN ,  WALKER JOEL R ,  HUNTLEY RAYMOND

IPC: A61K31/435 ,  A61K31/4353 ,  A61K31/4375 ,  C07D471/04

CPC classification number: A61K31/5377 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/506 ,  C07D471/04

Abstract: The present invention directs to a compound represented by Formula (I), comprising a 1,5-naphthyridine derivative. In one embodiment the 1,5-naphthyridine derivative of Formula (I) has an inhibitory activity against maternal embryonic leucine zipper kinase (MELK). The present invention also includes a method for preparing the 1,5-naphthyridine derivative of Formula (I). The present invention also includes a pharmaceutical composition containing the 1,5-naphthyridine derivative of Formula (I) as an active ingredient.

Abstract translation: 本发明涉及由式（I）表示的化合物，其包含1,5-萘啶衍生物。 在一个实施方案中，式（I）的1,5-萘啶衍生物对母体的亮氨酸亮氨酸拉链激酶（MELK）具有抑制活性。 本发明还包括制备式（I）的1,5-二氮杂萘衍生物的方法。 本发明还包含含有式（I）的1,5-二氮杂萘衍生物作为活性成分的药物组合物。

公开(公告)号：WO2008020596A3

公开(公告)日：2008-06-12

申请号：PCT/JP2007065873

申请日：2007-08-08

Applicant: ONCOTHERAPY SCIENCE INC ,  NAKAMURA YUSUKE ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

IPC: A61K31/7088 ,  A61K38/00 ,  A61K39/395 ,  A61P35/00 ,  C07K14/475 ,  C07K16/32 ,  C12N15/113 ,  C12Q1/68 ,  G01N33/53

CPC classification number: C12N15/1135 ,  A61K38/00 ,  C07K14/47 ,  C07K16/18 ,  C07K2317/56 ,  C07K2317/565 ,  C12N2310/111 ,  C12N2310/14 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158

Abstract: The invention features a method for inhibiting growth of a cancer cell by contacting the cell with a composition of an siRNA that inhibits expression of REG4 or KIAA0101. Methods of treating cancer are also within the invention. The invention also features products, including nucleic acid sequences and vectors as well as to compositions comprising them, useful in the provided methods. The invention also provides a method for inhibiting of tumor cell, for example pancreatic cancer cell, prostatic cancer cell, breast cancer cell, and bladder cancer cell, particularly pancreatic ductal adenocarcinoma (PDAC) by inhibiting REG4 gene. The present invention also relates to methods of treating or preventing PDAC in a subject comprising the step of administering to said subject a pharmaceutically effective amount of an antibody or fragment thereof that binds to a protein encoded by REG4. The present invention also relates to methods of diagnosing chemo-radiation therapeutic resistance of a cancer. The present invention also provides therapeutic agents or methods for treating cancer using the polypeptides. The polypeptides of the present invention are composed of an amino acid sequence which comprises polypeptide which comprises QKGIGEFF/SEQ ID NO: 21. The polypeptides of the present invention can be introduced into cancer cells by modifying the polypeptides with transfection agents such as poly-arginine.

Abstract translation: 本发明的特征在于通过使细胞与抑制REG4或KIAA0101表达的siRNA的组合物接触来抑制癌细胞生长的方法。 治疗癌症的方法也在本发明之内。 本发明的特征还在于提供的方法中有用的产品，包括核酸序列和载体以及包含它们的组合物。 本发明还提供了通过抑制REG4基因抑制肿瘤细胞，例如胰腺癌细胞，前列腺癌细胞，乳腺癌细胞和膀胱癌细胞，特别是胰腺导管腺癌（PDAC）的方法。 本发明还涉及在受试者中治疗或预防PDAC的方法，其包括向所述受试者施用药学有效量的与由REG4编码的蛋白质结合的抗体或其片段的步骤。 本发明还涉及诊断癌症的化学放射治疗抗性的方法。 本发明还提供了使用所述多肽治疗癌症的治疗剂或方法。 本发明的多肽由包含包含QKGIGEFF / SEQ ID NO：21的多肽的氨基酸序列组成。可以通过用转染剂如聚精氨酸修饰多肽将本发明的多肽引入癌细胞 。

公开(公告)号：WO2007116923A2

公开(公告)日：2007-10-18

申请号：PCT/JP2007057620

申请日：2007-03-29

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  DAIGO YATARO ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  DAIGO YATARO ,  NAKATSURU SHUICHI

IPC: C12N15/113

CPC classification number: C12N15/1138 ,  C12N2310/111 ,  C12N2310/14 ,  G01N33/57423 ,  G01N2500/02

Abstract: The present invention provides a method for assessing the prognosis of non-small cell lung cancer (NSCLC) using SEZ6L2, as well as methods for evaluating the efficacy of a particular therapy for NSCLC. In addition, the present invention provides kits for prognosing NSCLC. Furthermore, treatment of NSCLC cells with vector-based small interfering RNAs (siRNAs) against the SEZ6L2 gene suppressed its expression and resulted in growth suppression of the NSCLC cells. These results indicate that SEZ6L2 may be useful as a diagnostic marker and as a target for development of new molecular therapies for lung cancer.

Abstract translation: 本发明提供了一种使用SEZ6L2评估非小细胞肺癌（NSCLC）的预后的方法，以及用于评价特定治疗NSCLC的疗效的方法。 此外，本发明提供了用于预测NSCLC的试剂盒。 此外，针对SEZ6L2基因的基于载体的小干扰RNA（siRNA）治疗NSCLC细胞抑制其表达，并导致NSCLC细胞的生长抑制。 这些结果表明，SEZ6L2可能作为诊断标记和作为肺癌新型分子疗法开发的目标是有用的。

公开(公告)号：WO2006016525A3

公开(公告)日：2006-07-06

申请号：PCT/JP2005014369

申请日：2005-07-29

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  NAKATSURU SHUICHI

IPC: C12Q1/68 ,  C07K14/47 ,  C12N15/12

CPC classification number: C12Q1/6886 ,  C12Q2600/118 ,  C12Q2600/136 ,  C12Q2600/158

Abstract: The present application provides novel human genes B1194, A2282V1, A2282V2, and A2282V3 whose expression is markedly elevated in breast cancer. These genes and polypeptides encoded thereby can be used, for example, in the diagnosis of breast cancer, and as target molecules for developing drugs against breast cancer.

Abstract translation: 本申请提供了在乳腺癌中表达显着升高的新型人基因B1194，A2282V1，A2282V2和A2282V3。 由此编码的这些基因和多肽可用于例如乳腺癌的诊断，以及用于开发针对乳腺癌的药物的靶分子。

公开(公告)号：WO2005090603A3

公开(公告)日：2006-03-02

申请号：PCT/JP2005005613

申请日：2005-03-18

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  DAIGO YATARO ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  DAIGO YATARO ,  NAKATSURU SHUICHI

IPC: C12Q1/68 ,  A61K31/731

CPC classification number: A61K31/731 ,  C12Q1/6886 ,  C12Q2600/118 ,  C12Q2600/136 ,  C12Q2600/158

Abstract: Disclosed are methods for detecting non-small cell lung cancer (NSCLC) using differentially expressed genes KIF11, GHSR1b, NTSR1, and FOXM1. Also disclosed are methods of identifying compounds for treating and preventing NSCLC, based on the interaction between KOC1 and KIF11, or NMU and GHSR1b or NTSR1.

Abstract translation: 公开了使用差异表达基因KIF11，GHSR1b，NTSR1和FOXM1检测非小细胞肺癌（NSCLC）的方法。 还公开了基于KOC1和KIF11或NMU和GHSR1b或NTSR1之间的相互作用鉴定用于治疗和预防NSCLC的化合物的方法。

公开(公告)号：WO2005083118A2

公开(公告)日：2005-09-09

申请号：PCT/JP2005002090

申请日：2005-02-04

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

IPC: C12Q1/68 ,  G01N33/574

CPC classification number: C12Q1/6886 ,  A61K39/0011 ,  C12Q2600/136 ,  G01N33/57434 ,  G01N2500/10

Abstract: Objective methods for diagnosing a predisposition to developing prostate cancer (PRC) are described herein. In one embodiment, the diagnostic method involves the determining a expression level of PRC -associated gene that discriminate between PRC and PIN. The present invention further provides methods of screening for therapeutic agents useful in the treatment of PRC, methods of treating PRC.

Abstract translation: 本文描述了诊断发展中的前列腺癌（PRC）倾向的客观方法。 在一个实施方案中，诊断方法涉及确定区分PRC和PIN的PRC相关基因的表达水平。 本发明还提供筛选用于治疗PRC的治疗剂的方法，以及治疗PRC的方法。

公开(公告)号：WO2004031231A3

公开(公告)日：2004-07-08

申请号：PCT/JP0312074

申请日：2003-09-22

Applicant: ONCOTHERAPY SCIENCE INC ,  JAPAN AS REPRESENTED BY THE PR ,  NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  NAKAGAWA HIDEWAKI ,  NAKATSURU SHUICHI

IPC: C07K14/47 ,  C12Q1/68

CPC classification number: C07K14/47 ,  C12Q1/6886 ,  C12Q2600/136

Abstract: The present application provides novel human gene MICAL2-PV whose expression is markedly elevated in prostate cancers. Furthermore, it provides polypeptides encoded by the gene as well as polypeptides encoded by PCOTH which expression was also discovered to be elevated in prostate cancers. The genes and polypeptides encoded by the genes can be used, for example, in the diagnosis of prostate cancers, as target molecules for developing drugs against the disease, and for attenuating cell growth of prostate cancer.

Abstract translation: 本申请提供了新型人基因MICAL2-PV，其表达在前列腺癌中显着升高。 此外，它提供由该基因编码的多肽以及由PCOTH编码的多肽，其表达也被发现在前列腺癌中升高。 由该基因编码的基因和多肽可以用于例如前列腺癌的诊断中，作为用于开发针对该疾病的药物的靶分子，以及用于减轻前列腺癌的细胞生长。

公开(公告)号：WO2007013358A3

公开(公告)日：2007-07-05

申请号：PCT/JP2006314442

申请日：2006-07-14

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  INAKI KOICHIRO

Inventor： NAKAMURA YUSUKE ,  KATAGIRI TOYOMASA ,  INAKI KOICHIRO

IPC: C07K7/04 ,  A61K38/10 ,  A61K38/17 ,  C07K7/08 ,  C07K14/435 ,  C12N15/62 ,  G01N33/50

CPC classification number: G01N33/57438 ,  A61K38/08 ,  A61K38/10 ,  A61K38/1709 ,  C07K14/47 ,  G01N33/5011 ,  G01N33/6893 ,  G01N2500/00

Abstract: The present invention provides polypeptides useful for treating and preventing cancer. The present invention also provides therapeutic agents or methods for treating cancer using the polypeptides. The polypeptides of the present invention are composed of an amino acid sequence which comprises VIVIT and is preferably a polypeptide in which the motif sequence PxIxIT at positions 37 to 41 of the amino acid sequence of the C1958 protein (SEQ ID NO: 2) is replaced with PVIVIT. The polypeptides of the present invention can be introduced into cancer cells by modifying the polypeptides with transfection agents such as poly-arginine. The present invention provides methods and kits for identifying inhibitors of the interaction between C1958 and PPP3CA which find utility in the treatment and prevention of cancer. Also disclosed herein are compositions for treating or preventing cancer identified by the screening method of the present invention and methods of using same in the treatment and prevention of cancer.

Abstract translation: 本发明提供了可用于治疗和预防癌症的多肽。 本发明还提供了使用多肽治疗癌症的治疗剂或方法。 本发明的多肽由包含VIVIT的氨基酸序列组成，优选其中C1958蛋白（SEQ ID NO：2）的氨基酸序列的第37至41位上的基序序列PxIxIT被替换的多肽 与PVIVIT。 本发明的多肽可以通过用转染试剂例如聚精氨酸修饰多肽而被引入到癌细胞中。 本发明提供用于鉴定C1958和PPP3CA之间相互作用的抑制剂的方法和试剂盒，其可用于治疗和预防癌症。 本文还公开了用于治疗或预防由本发明的筛选方法鉴定的癌症的组合物及其在治疗和预防癌症中的使用方法。

公开(公告)号：WO2007013359A3

公开(公告)日：2007-06-14

申请号：PCT/JP2006314443

申请日：2006-07-14

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  FURUKAWA YOICHI ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  FURUKAWA YOICHI ,  NAKATSURU SHUICHI

IPC: C12Q1/68

CPC classification number: C12Q1/6886 ,  C12Q2600/136

Abstract: The present invention provides methods for detecting and diagnosing cancer. According to an embodiment, the diagnostic method involves the determination of the expression level of the RASGEF1A gene which was discovered to discriminate cancer cells from normal cells. Furthermore, the present invention provides methods of screening for therapeutic agents useful in the treatment of cancer, methods for treating cancer, and methods for vaccinating a subject against cancer.

Abstract translation: 本发明提供了检测和诊断癌症的方法。 根据一个实施方案，诊断方法包括确定被发现鉴别癌细胞与正常细胞的RASGEF1A基因的表达水平。 此外，本发明提供筛选可用于治疗癌症的治疗剂的方法，用于治疗癌症的方法，以及用于接种受试者接种癌症的方法。

公开(公告)号：WO2007004526A3

公开(公告)日：2007-05-10

申请号：PCT/JP2006313038

申请日：2006-06-23

Applicant: ONCOTHERAPY SCIENCE INC ,  UNIV TOKYO ,  NAKAMURA YUSUKE ,  FURUKAWA YOICHI ,  HAMAMOTO RYUJI ,  NAKATSURU SHUICHI

Inventor： NAKAMURA YUSUKE ,  FURUKAWA YOICHI ,  HAMAMOTO RYUJI ,  NAKATSURU SHUICHI

IPC: C12Q1/48 ,  A61K38/00 ,  A61P35/00 ,  G01N33/68

CPC classification number: G01N33/5011 ,  C12Q1/48 ,  C12Y201/01043 ,  G01N33/57407 ,  G01N2333/4736 ,  G01N2333/91011 ,  G01N2500/02

Abstract: The present invention features a method for determining the methyltransferase activity of a polypeptide and screening for modulators of methyltransferase activity, more particularly for modulators of the methylation of retinoblastoma by SMYD3. The invention further provides a method or pharmaceutical composition for prevention or treating of colorectal cancer, hepatocellular carcinoma, bladder cancer and/or breast cancer using a modulator so identified. N-terminal truncated forms of SMYD3 (alias ZNFN3A1) have higher methylating activity. Lys 824 is a preferred methylation site on the RB1 protein for SMYD3.

Abstract translation: 本发明的特征在于确定多肽的甲基转移酶活性并筛选甲基转移酶活性的调节剂的方法，更特别是用于通过SMYD3进行视网膜母细胞瘤甲基化的调节剂。 本发明还提供了使用所鉴定的调节剂预防或治疗结肠直肠癌，肝细胞癌，膀胱癌和/或乳腺癌的方法或药物组合物。 SMYD3（别名ZNFN3A1）的N-末端截短形式具有较高的甲基化活性。 Lys 824是SMYD3的RB1蛋白上优选的甲基化位点。