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    Photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy
    1.
    发明授权
    Photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy 有权
    基于聚合物衍生物的光敏剂 - 用于光动力疗法的光敏剂共轭物

    公开(公告)号：US08614285B2

    公开(公告)日：2013-12-24

    申请号：US12595103

    申请日：2008-04-23

    Applicant: Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Jong-Ho Kim ,  Kyeong-Soon Park

    Inventor： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Jong-Ho Kim ,  Kyeong-Soon Park

    IPC: C08F251/00 ,  A61K31/555

    CPC classification number: A61K41/0071 ,  A61K47/61 ,  A61K47/6929

    Abstract: Disclosed is a novel photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy capable of being selectively accumulated in cancerous tissues and producing singlet oxygen or free radical by laser irradiation. The polymer derivatives-photosensitizer conjugates for photodynamic therapy are prepared as nano-sized particles, and have excellent selection and accumulation ratio for cancerous tissues. The photosensitizer conjugates can produce singlet oxygen or free radical by a specific laser wavelength. Owing to the excellent selection and accumulation ratio for cancerous tissues, the conjugates minimizes photo-cytotoxicity of the conventional photosensitizer having a low molecular amount. Accordingly, the conjugates are very useful as a photosensitizes for photodynamic therapy with reduced side effects and excellent therapeutic effectiveness.

    Abstract translation: 公开了一种基于用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物的新型光敏剂，其能够选择性地积累在癌组织中并通过激光照射产生单线态氧或自由基。 用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物制备为纳米尺寸颗粒，并且对于癌组织具有优异的选择和积累比。 光敏剂共轭物可以通过特定的激光波长产生单线态氧或自由基。 由于癌组织的优异的选择和积累比，共轭物使具有低分子量的常规光敏剂的光细胞毒性最小化。 因此，缀合物对于具有降低的副作用和优异治疗有效性的光动力疗法的光敏剂是非常有用的。

    NANOPARTICLE SENSOR FOR MEASURING PROTEASE ACTIVITY AND METHOD FOR MANUFACTURING THE SAME
    2.
    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

    Applicant: 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

    Inventor： 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: C07K9/00 ,  B82Y5/00

    CPC classification number: C12Q1/37 ,  G01N33/54346 ,  Y10S977/773 ,  Y10S977/774 ,  Y10S977/807 ,  Y10S977/811 ,  Y10S977/953

    Abstract: 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.

    Abstract translation: 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。

    Gold nanoparticle based protease imaging probes and use thereof
    4.
    发明授权
    Gold nanoparticle based protease imaging probes and use thereof 有权
    基于金纳米颗粒的蛋白酶成像探针及其用途

    公开(公告)号：US08551727B2

    公开(公告)日：2013-10-08

    申请号：US12595078

    申请日：2008-04-10

    Applicant: Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  Cheol-Hee Ahn ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park

    Inventor： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  Cheol-Hee Ahn ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park

    IPC: C12Q1/37 ,  C12Q1/34 ,  B82B3/00 ,  C12N11/14 ,  C12N11/18

    CPC classification number: A61K49/0056 ,  A61K49/0032 ,  A61K49/0065 ,  A61K49/0093 ,  C12Q1/37

    Abstract: Disclosed are a metal nanoparticle onto which a peptide substrate specifically degraded by protease and fluorophore are chemically modified for selectively imaging protease expressed in cell and in tissue in a human body, and the use thereof. Also, a quantitative analysis method of protease using the metal nanoparticle, a cell imaging method and a drug screening method of inhibiting a protease overexpression are provided. In detail, the present invention is directed to a metal nanoparticle having a peptide substrate and fluorophore coupled thereto, the peptide substrate and the fluorophore being specifically degraded by due to a protease activated in various ways in cell and in a human body to exhibit fluorescence. Hence, the metal nanoparticle can be used to rapidly screen activation and inhibition of the protease in the imaging manner. Also, the metal nanoparticle is capable of being selectively absorbed into a cell and a tissue so as to be possibly used as a sensor for real-time cell imaging and early diagnosis of non-invasive diseases.

    Abstract translation: 公开了一种金属纳米颗粒，其上通过蛋白酶和荧光团特异性降解的肽底物被化学修饰以选择性地成像在细胞和人体组织中表达的蛋白酶及其用途。 另外，提供了使用金属纳米粒子的蛋白酶的定量分析方法，细胞成像方法和抑制蛋白酶过表达的药物筛选方法。 详细地说，本发明涉及一种具有肽底物和与其连接的荧光团的金属纳米颗粒，肽底物和荧光团由于在细胞和人体中以各种方式活化的蛋白酶而被特异性地降解以显示出荧光。 因此，金属纳米颗粒可用于以成像方式快速筛选蛋白酶的活化和抑制。 此外，金属纳米粒子能够被选择性地吸收到细胞和组织中，以便可能用作用于实时细胞成像和非侵入性疾病的早期诊断的传感器。

    GOLD NANOPARTICLE BASED PROTEASE IMAGING PROBES AND USE THEREOF
    6.
    发明申请
    GOLD NANOPARTICLE BASED PROTEASE IMAGING PROBES AND USE THEREOF 有权
    基于金纳米粒子的蛋白成像探针及其应用

    公开(公告)号：US20100124757A1

    公开(公告)日：2010-05-20

    申请号：US12595078

    申请日：2008-04-10

    Applicant: Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  Cheol-Hee Ahn ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park

    Inventor： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  Cheol-Hee Ahn ,  In-Chan Youn ,  Seul-Ki Lee ,  Kyeong-Soon Park

    IPC: C12Q1/37 ,  C07K2/00

    CPC classification number: A61K49/0056 ,  A61K49/0032 ,  A61K49/0065 ,  A61K49/0093 ,  C12Q1/37

    Abstract: Disclosed are a metal nanoparticle onto which a peptide substrate specifically degraded by protease and fluorophore are chemically modified for selectively imaging protease expressed in cell and in tissue in a human body, and the use thereof. Also, a quantitative analysis method of protease using the metal nanoparticle, a cell imaging method and a drug screening method of inhibiting a protease overexpression are provided. In detail, the present invention is directed to a metal nanoparticle having a peptide substrate and fluorophore coupled thereto, the peptide substrate and the fluorophore being specifically degraded by due to a protease activated in various ways in cell and in a human body to exhibit fluorescence. Hence, the metal nanoparticle can be used to rapidly screen activation and inhibition of the protease in the imaging manner. Also, the metal nanoparticle is capable of being selectively absorbed into a cell and a tissue so as to be possibly used as a sensor for real-time cell imaging and early diagnosis of non-invasive diseases.

    Abstract translation: 公开了一种金属纳米颗粒，其上通过蛋白酶和荧光团特异性降解的肽底物被化学修饰以选择性地成像在细胞和人体组织中表达的蛋白酶及其用途。 另外，提供了使用金属纳米粒子的蛋白酶的定量分析方法，细胞成像方法和抑制蛋白酶过表达的药物筛选方法。 详细地说，本发明涉及一种具有肽底物和与其连接的荧光团的金属纳米颗粒，肽底物和荧光团由于在细胞和人体中以各种方式活化的蛋白酶而被特异性地降解以显示出荧光。 因此，金属纳米颗粒可用于以成像方式快速筛选蛋白酶的活化和抑制。 此外，金属纳米粒子能够被选择性地吸收到细胞和组织中，以便可能用作用于实时细胞成像和非侵入性疾病的早期诊断的传感器。

    Human serum albumin-siRNA nano-sized carrier system
    7.
    发明授权
    Human serum albumin-siRNA nano-sized carrier system 有权
    人血清白蛋白siRNA siRNA纳米载体体系

    公开(公告)号：US08513402B2

    公开(公告)日：2013-08-20

    申请号：US13245180

    申请日：2011-09-26

    Applicant: Kwangmeyung Kim ,  Ick Chan Kwon ,  Kuiwon Choi ,  In Chan Youn ,  MyungSook Huh ,  Sojin Lee

    Inventor： Kwangmeyung Kim ,  Ick Chan Kwon ,  Kuiwon Choi ,  In Chan Youn ,  MyungSook Huh ,  Sojin Lee

    IPC: C07H21/04

    CPC classification number: C12N15/111 ,  A61K47/643 ,  C12N2320/32

    Abstract: Disclosed are a human serum albumin-siRNA carrier system having siRNA bound to human serum albumin and a user thereof, and especially, human serum albumin-siRNA carrier system, which has a biodegradable covalent bond between human serum albumin polymer and siRNA and is stable in a living body, and a user thereof.The human serum albumin-siRNA carrier system having the biodegradable covalent bond between the human serum albumin and the siRNA exhibits high siRNA delivery efficiency to a target site in the living body. Therefore, the human serum albumin-siRNA carrier system may allow siRNA for therapy to be efficiently delivered to a target site such as cancer tissues in the living body even by being administrated in a relatively low concentration, which may result in a wide use for therapies of various diseases.

    Abstract translation: 公开了具有与人血清白蛋白结合的siRNA及其使用者的人血清白蛋白-siRNA载体体系，特别是人血清白蛋白-siRNA载体体系，其在人血清白蛋白聚合物和siRNA之间具有可生物降解的共价键，并且在 生物体及其使用者。 在人体血清白蛋白和siRNA之间具有可生物降解的共价键的人血清白蛋白-siRNA载体体系对生物体中的靶位点显示出高的siRNA递送效率。 因此，人体血清白蛋白-siRNA载体体系可以使siRNA用于治疗有效地递送到目标部位如生物体中的癌组织，甚至通过以相对低的浓度施用，这可能导致广泛用于治疗 的各种疾病。

    NOVEL PHOTOSENSITIZER BASED ON POLYMER DERIVATIVES-PHOTOSENSITIZER CONJUGATES FOR PHOTODYNAMIC THERAPY
    8.
    发明申请
    NOVEL PHOTOSENSITIZER BASED ON POLYMER DERIVATIVES-PHOTOSENSITIZER CONJUGATES FOR PHOTODYNAMIC THERAPY 有权
    基于聚合物衍生物的新型光敏剂 - 光致变色治疗光敏剂

    公开(公告)号：US20100222538A1

    公开(公告)日：2010-09-02

    申请号：US12595103

    申请日：2008-04-23

    Applicant: Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Jong-Ho Kim ,  Kyeong-Soon Park

    Inventor： Ick-Chan Kwon ,  Kui-Won Choi ,  Kwang-Meyung Kim ,  In-Chan Youn ,  Jong-Ho Kim ,  Kyeong-Soon Park

    IPC: C08F251/00

    CPC classification number: A61K41/0071 ,  A61K47/61 ,  A61K47/6929

    Abstract: Disclosed is a novel photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy capable of being selectively accumulated in cancerous tissues and producing singlet oxygen or free radical by laser irradiation. The polymer derivatives-photosensitizer conjugates for photodynamic therapy are prepared as nano-sized particles, and have excellent selection and accumulation ratio for cancerous tissues. The photosensitizer conjugates can produce singlet oxygen or free radical by a specific laser wavelength. Owing to the excellent selection and accumulation ratio for cancerous tissues, the conjugates minimizes photo-cytotoxicity of the conventional photosensitizer having a low molecular amount. Accordingly, the conjugates are very useful as a photosensitizes for photodynamic therapy with reduced side effects and excellent therapeutic effectiveness.

    Abstract translation: 公开了一种基于用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物的新型光敏剂，其能够选择性地积累在癌组织中并通过激光照射产生单线态氧或自由基。 用于光动力学治疗的聚合物衍生物 - 光敏剂共轭物制备为纳米尺寸颗粒，并且对于癌组织具有优异的选择和积累比。 光敏剂共轭物可以通过特定的激光波长产生单线态氧或自由基。 由于癌组织的优异的选择和积累比，共轭物使具有低分子量的常规光敏剂的光细胞毒性最小化。 因此，缀合物对于具有降低的副作用和优异治疗有效性的光动力疗法的光敏剂是非常有用的。

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