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    METHOD FOR SCREENING ANTICANCER AGENT INHIBITING BINDING OF AIMP2-DX2 AND HSP70
    3.
    发明公开
    METHOD FOR SCREENING ANTICANCER AGENT INHIBITING BINDING OF AIMP2-DX2 AND HSP70 审中-公开

    公开(公告)号：EP3418739A1

    公开(公告)日：2018-12-26

    申请号：EP17763538.0

    申请日：2017-03-07

    申请人： Medicinal Bioconvergence Research Center

    发明人： KIM, Sunghoon ,  KIM, Dae Gyu ,  LIM, Semi

    IPC分类号： G01N33/50 ,  G01N33/574 ,  A61K48/00 ,  A61K31/5377 ,  A61K31/404

    CPC分类号： A61K31/404 ,  A61K31/5377 ,  A61K48/00 ,  G01N33/50 ,  G01N33/574

    摘要： The present invention relates to a method for screening an anticancer agent which inhibits the binding of AIMP2-DX2 and HSP70. More particularly, the present invention relates to a method for screening an anticancer agent and an anticancer composition comprising an anticancer agent screened by the method as an active ingredient, the method comprising: a step of contacting AIMP2-DX2 or a fragment thereof with HSP70 of a fragment thereof in the presence or absence of a test substance; a step of measuring the binding of AIMP2-DX2 and HSP70; a step of determining a change in the level of binding of AIMP2-DX2 and HSP70 by the test substance; a step of screening a test substance which reduces the level of binding of AIMP2-DX2 and HSP70; and a step of identifying an anticancer activity of the screened test substance in cells or animals. The present invention can be effectively used to develop an anticancer agent with a completely new mechanism of action on the basis of the discovery that HSP70 is a regulator that directly binds to and stabilizes AIMP2-DX3, which is important for cancer development and progression. In addition, the pharmaceutical composition for preventing or treating cancer comprising, as an active ingredient, an anticancer agent screened according to the method of the present invention inhibits the expression of HSP70 or inhibits the binding of HSP70 and AIMP2-DX2, thereby lowering the level of AIMP2-DX2 protein, and can effectively prevent the progression of cancer. As such, the pharmaceutical composition can be useful for developing a cancer treating agent.

    NOVEL PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER
    4.
    发明公开
    NOVEL PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER 审中-公开
    药剂师ZUSAMMENSETZUNG ZUR VORBEUGUNG UND BEHANDLUNG VON KREBS

    公开(公告)号：EP3020399A1

    公开(公告)日：2016-05-18

    申请号：EP14810113.2

    申请日：2014-06-11

    申请人： Medicinal Bioconvergence Research Center

    发明人： KIM, Sunghoon ,  KWON, Nam Hoon ,  KIM, Dae Gyu

    IPC分类号： A61K31/357 ,  A61P35/00

    CPC分类号： A61K31/395 ,  C07D273/01

    摘要： The present invention relates to a novel anticancer composition, and more specifically, to: an anticancer pharmaceutical composition comprising a compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof; a method for preventing or treating cancer, comprising a step of administering an effective amount of a compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof to an individual in need thereof; and a use of a compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof for preparing an agent for preventing or treating cancer. The compound of the present invention inhibits, dependent on the concentration, the protein level of AIMP2-DX2, which is overexpressed in lung cancer cells, and inhibits, dependent on the concentration, the survival of cancer cells without acting on normal cells, and thus a pharmaceutical composition comprising the compound of the present invention or a pharmaceutically acceptable salt thereof can be used for preventing and treating cancer.

    摘要翻译： 本发明涉及一种新型抗癌组合物，更具体地涉及：含有由化学式1表示的化合物或其药学上可接受的盐的抗癌药物组合物; 预防或治疗癌症的方法，包括向有需要的个体施用有效量的由化学式1表示的化合物或其药学上可接受的盐的步骤; 以及由化学式1表示的化合物或其药学上可接受的盐在制备用于预防或治疗癌症的药剂中的用途。 本发明化合物根据浓度抑制在肺癌细胞中过表达的AIMP2-DX2的蛋白质水平，并且依赖于浓度而不影响癌细胞的存活而不作用于正常细胞，因此 包含本发明化合物或其药学上可接受的盐的药物组合物可用于预防和治疗癌症。

    METHOD FOR SCREENING CANCER METASTASIS INHIBITOR USING CULTURE OF CELLS OR SPHEROIDICALLY AGGREGATED CELLS IN WHICH LYSYL-TRNA SYNTHETASE IS REGULATED TO BE EXPRESSED OR UNEXPRESSED
    5.
    发明公开
    METHOD FOR SCREENING CANCER METASTASIS INHIBITOR USING CULTURE OF CELLS OR SPHEROIDICALLY AGGREGATED CELLS IN WHICH LYSYL-TRNA SYNTHETASE IS REGULATED TO BE EXPRESSED OR UNEXPRESSED 审中-公开
    方法癌转移抑制剂参考细胞或球形聚集细胞具有调节赖氨酰tRNA合成酶的表达或不表达的文化筛选

    公开(公告)号：EP3006941A1

    公开(公告)日：2016-04-13

    申请号：EP14797157.6

    申请日：2014-05-13

    申请人： Medicinal Bioconvergence Research Center

    发明人： LEE, Jung Weon ,  KIM, Sunghoon ,  NAM, Seo-Hee ,  KIM, Dae Gyu

    IPC分类号： G01N33/574 ,  C12Q1/68 ,  C12M1/34 ,  C12M3/00

    CPC分类号： G01N33/573 ,  C12Q1/6886 ,  C12Q2600/112 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N33/5011 ,  G01N33/574 ,  G01N33/57419 ,  G01N2333/4704 ,  G01N2333/9015 ,  G01N2500/00 ,  G01N2500/04 ,  G01N2500/10

    摘要： The present invention relates to a method for scanning a cancer metastasis inhibitor by analyzing the activity of lysyl-tRNA synthetase (KRS) in a cancer cell line cultured in a three-dimensional collagen gel environment, and to a method for monitoring the dissemination of cancer cells from aggregated cancer cells, and the epithelial-mesenchymal transition, migration, invasion, and metastasis of cancer cells. Specifically, it was verified that, in the case where a cell line or a spheroidically aggregated cell line, in which KRS has been regulated to be expressed or unexpressed, was constructed by using various colorectal cancer cells including HCT116 cell line and then cultured in a two-dimensional environment, the incomplete epithelial-to-mesenchymal transition phenotype (incomplete ECM phenotype) was induced in the cell line inhibiting KRS expression, and the inhibition of KRS expression inhibited cell-extracellular matrix (ECM) adhesion and cell-ECM signaling activity. In addition, it was verified that, in the case where the constructed spheroid cell line was cultured in an aqueous environment or a three-dimensional collage gel culture environment, the inhibition of KRS expression induced cells into mesenchymal cells but failed to reach the disintegration of cell-cell adhesion; inhibited the cell-ECM adhesion and the related signaling activity, causing the inhibition of the dissemination of cells from spheroid cells cultured in a three-dimensional collagen gel culture environment; and failed to induce the dissemination of cells through TGFβ1 present in the cellular microenvironment. Thus, the present invention can be used as a method for screening a cancer metastasis inhibitor and a method for monitoring the migration, invasion and metastasis of cancer cells, and will be useful as one of the screening methods capable of creating low-cost, high-efficient added value at the time of pre-clinical tests required for drug development.

    摘要翻译： 本发明涉及一种用于通过在三维胶原凝胶环境培养的癌细胞系分析赖氨酰-tRNA合成酶（KRS）的活性扫描癌转移抑制剂，以及用于监控癌症的传播的方法 细胞从聚集的癌细胞，和上皮 - 间充质转换，迁移，侵入，和癌细胞的转移。 具体而言，什么证实，在的情况下待表达的细胞系或一个spheroidically聚集细胞系，其中KRS已调节或不表达什么通过使用各种结直肠癌细胞，包括HCT116细胞系，然后在培养的构筑 二维环境下，不完全的上皮 - 间充质在细胞系中抑制KRS表达从而诱发转变表型（不完全的ECM表型），以及KRS表达的抑制抑制细胞 - 细胞外基质（ECM）的粘附和细胞-ECM信号活动 ， 此外，它什么证实，在的情况下，其在wässrige环境培养在所构造的旋转椭圆体细胞系或三维拼贴凝胶培养环境，KRS表达诱导细胞的抑制成间充质细胞，但未能达到的崩解 粘附的细胞 - 细胞; 抑制细胞-ECM粘附和相关的信号转导活性，导致从在三维胶原蛋白凝胶中培养环境中培养球体细胞的细胞传播的抑制; 并不能诱导细胞通过TGF²1本传播中细胞微环境。 因此，本发明可以被用作用于筛选癌转移抑制剂以及用于监测癌症细胞的迁移，侵袭和转移的方法的方法，并且将是有用的作为能够产生低成本的，高的筛选方法之一 在效率高达用于药物开发所需的前期临床试验的时间增值。

    USE OF A NOVEL AMINOPYRIDINE DERIVATIVE TO PREVENT OR TREAT CANCER
    6.
    发明公开
    USE OF A NOVEL AMINOPYRIDINE DERIVATIVE TO PREVENT OR TREAT CANCER 审中-公开
    VERWENDUNG EINES NEUARTIGEN AMINOPYRIDINDERIVATS ZUR VORBEUGUNG ODER BEHANDLUNG VON KREBS

    公开(公告)号：EP2840081A1

    公开(公告)日：2015-02-25

    申请号：EP13778232.2

    申请日：2013-04-19

    申请人： Medicinal Bioconvergence Research Center

    发明人： KIM, Sunghoon ,  LEE, Hee Sook ,  OH, Young Sun ,  KIM, Dae Gyu

    IPC分类号： C07D213/75 ,  C07D215/38 ,  A61K31/435 ,  A61P35/00

    CPC分类号： C07D215/38 ,  A61K31/435 ,  C07D213/75

    摘要： The present invention relates to the use of a novel aminopyridine derivative to prevent or treat cancer, and more particularly to a carcinostatic composition including a compound of Formula 1 or a derivative thereof as an active principle. The compound of the present invention degrades the activation of AIMP2-D7C2 targeted by a novel anticancer drug so as to effectively in-duce destruction of cancer cells, thus effecting prevention and treatment of cancer. Therefore the compound of the present invention can be used to prevent and treat cancer.

    摘要翻译： 本发明涉及新型氨基吡啶衍生物用于预防或治疗癌症的用途，更具体地涉及包含式1化合物或其衍生物作为活性成分的制癌组合物。 本发明的化合物降低了由新型抗癌药物靶向的AIMP2-D7C2的活化，有效地降低了癌细胞的破坏，从而进行了癌症的预防和治疗。 因此，本发明的化合物可用于预防和治疗癌症。