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    NANOPARTICLE SENSOR FOR MEASURING PROTEASE ACTIVITY AND METHOD FOR MANUFACTURING THE SAME
    4.
    发明申请
    NANOPARTICLE SENSOR FOR MEASURING PROTEASE ACTIVITY AND METHOD FOR MANUFACTURING THE SAME 有权
    用于测量蛋白酶活性的纳米颗粒传感器及其制造方法

    公开(公告)号：US20110213121A1

    公开(公告)日：2011-09-01

    申请号：US13060902

    申请日：2009-08-27

    申请人： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park ,  Dae-Hyuk Moon ,  Dae-Yoon Chi ,  Seung-Jin Lee ,  Seung-Jae Myung

    发明人： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park ,  Dae-Hyuk Moon ,  Dae-Yoon Chi ,  Seung-Jin Lee ,  Seung-Jae Myung

    IPC分类号： C07K9/00 ,  B82Y5/00

    CPC分类号： C12Q1/37 ,  G01N33/54346 ,  Y10S977/773 ,  Y10S977/774 ,  Y10S977/807 ,  Y10S977/811 ,  Y10S977/953

    摘要： Disclosed are a nanoparticle sensor for measuring protease activity, for protease imaging, and a method for preparing the same. More specifically, the present invention relates to a nanoparticle sensor for measuring protease activity in which a fluorophore- and a quencher-conjugated peptide substrate is conjugated to a biocompatible polymer nanoparticle. The peptide substrate is specifically lysed by a protease. The sensor according to the present invention is capable of inhibiting emission of fluorescence with high extinctive activity of the quencher on a fluorescent material. But strong fluorescence is specifically emitted only if the peptide substrate is lysed by a specific protease. Therefore, the sensor is especially useful as a method for screening a novel drug such as a protease overexpression inhibitor, and early diagnosis of incurable diseases and various diseases such as autoimmune diseases including cancer, osteoarthritis, rheumatoid arthritis and dementia.

    摘要翻译： 公开了用于测定蛋白酶活性的蛋白酶成像用纳米粒子传感器及其制备方法。 更具体地，本发明涉及用于测量蛋白酶活性的纳米颗粒传感器，其中荧光团和猝灭剂缀合的肽底物与生物相容性聚合物纳米颗粒缀合。 肽底物被蛋白酶特异性裂解。 根据本发明的传感器能​​够抑制荧光材料上猝灭剂具有高灭绝活性的荧光发射。 但是如果肽底物被特异性蛋白酶裂解，则强荧光是特异性发射的。 因此，该传感器作为筛选新型药物如蛋白酶过表达抑制剂的方法，以及早期诊断不治之症以及各种疾病，如自身免疫性疾病，包括癌症，骨关节炎，类风湿性关节炎和痴呆症，都是特别有用的。

    1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES HAVING EFFECTS OF PREVENTING AND TREATING DEGENERATIVE AND INFLAMMATORY DISEASES
    6.
    发明申请
    1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES HAVING EFFECTS OF PREVENTING AND TREATING DEGENERATIVE AND INFLAMMATORY DISEASES 审中-公开
    具有预防和治疗衰老和炎症疾病的作用的1,2,3,4-四氢喹啉衍生物

    公开(公告)号：US20100217003A1

    公开(公告)日：2010-08-26

    申请号：US12518068

    申请日：2007-12-10

    申请人： On-You Hwang ,  Dae-Yoon Chi ,  Hyo-Jin Son ,  Jai-Woong Seo

    发明人： On-You Hwang ,  Dae-Yoon Chi ,  Hyo-Jin Son ,  Jai-Woong Seo

    IPC分类号： C07D217/04

    CPC分类号： A61K31/472

    摘要： Provided are 7-hydroxy-6-methoxy-1,2,3,4-tetrahydroisoquinoline derivatives and synthesis methods thereof. The compounds significantly inhibit the production of nitrogen monoxide (NO) and superoxide in an activated microglial cell and expressions of TNF-α, IL-1β inducive NO synthase and cyclooxygenase-2 genes. They also prevent NF-kB shift to a nucleus, decrease reactive oxygen species (ROS), inhibit expression of GTP cyclohydrolase I gene and over-production of tetrahydrobiopterin (BH4), and protect dopaminergic neurons from injury due to activated microglial cells. Consequently, the compounds are effective in treating inflammatory and neurodegenerative diseases.

    摘要翻译： 提供7-羟基-6-甲氧基-1,2,3,4-四氢异喹啉衍生物及其合成方法。 该化合物显着抑制活化的小胶质细胞中一氧化氮（NO）和超氧化物的产生以及TNF-α，IL-1和bgr的表达。 诱导性NO合成酶和环氧合酶-2基因。 它们还可以阻止NF-kB转移到细胞核，减少活性氧（ROS），抑制GTP环化水解酶I基因的表达和四氢生物喋呤（BH4）的过量产生，并保护多巴胺能神经元免受活化的小胶质细胞的损伤。 因此，这些化合物有效地治疗炎性和神经退行性疾病。