公开(公告)号：US10213515B2

公开(公告)日：2019-02-26

申请号：US15169493

申请日：2016-05-31

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Kwangmeyung Kim ,  Ju Hee Ryu ,  Ick Chan Kwon ,  Man Kyu Shim ,  Hong Yeol Yoon

IPC: A61K51/00 ,  A61M36/14 ,  A61K49/00 ,  C07K9/00 ,  G01N33/574 ,  G01N33/58 ,  C07K5/11 ,  C07K5/107 ,  A61K47/54

Abstract: The present disclosure relates to a glycopeptide targeting cancer cells and a contrast agent kit containing the same. The glycopeptide is one wherein an azide reporting monosaccharide is bound to a substrate peptide. As the substrate peptide is specifically cleaved by cathepsin B in cancer cells, an azide reporting monosaccharide is expressed onto the cell surface via metabolic glycoengineering, thereby providing a target for action as a contrast agent. Accordingly, because the azide is exposed to the cell surface only by cathepsin B, as it is specifically expressed in cancer cells, in particular in metastatic cancer cells, while it is limitedly expressed in normal cells and is hardly excreted out the cells, the cancer cells can be selectively imaged by an azide-specific contrast agent.

公开(公告)号：US20190010528A1

公开(公告)日：2019-01-10

申请号：US16026796

申请日：2018-07-03

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Hak Suk Chung ,  Yu Hyun Ji ,  Jin Su An ,  Ick Chan Kwon ,  Eun Gyeong Yang

IPC: C12P19/12 ,  C12N9/16 ,  C12N9/14

Abstract: A bacterium that constitutively produces monophosphoryl lipid A (MLA) and a method of producing MLA by using the bacterium may simply produce MLA and a derivative thereof without acid hydrolysis, reduce a probability of natural mutation, and increase yields of MLA and a derivative thereof by constitutive expression of the MLA and derivative thereof.

公开(公告)号：US09801943B2

公开(公告)日：2017-10-31

申请号：US13774247

申请日：2013-02-22

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Kwang Meyung Kim ,  Ick Chan Kwon ,  Kuiwon Choi ,  Heebeom Koo ,  Sang-min Lee ,  Inchan Youn

IPC: A61K47/26 ,  A61K47/34 ,  A61K47/48 ,  A61K49/00

CPC classification number: A61K47/26 ,  A61K47/34 ,  A61K47/549 ,  A61K47/555 ,  A61K47/6911 ,  A61K49/0032 ,  A61K49/0052

Abstract: The present disclosure relates to a method for in vivo targeting of a nanoparticle via bioorthogonal copper-free click chemistry, more particularly to a method for in vivo targeting of a nanoparticle, including: injecting a precursor capable of being metabolically engineered in vivo when injected into a living system and having a first bioorthogonal functional group into the living system; and injecting a nanoparticle having a second bioorthogonal functional group which can perform a bioorthogonal copper-free click reaction with the first bioorthogonal functional group attached thereto into the living system.In accordance with the present disclosure, accumulation of nanoparticles at a target site in a living system can be increased remarkably and the biodistribution of the nanoparticles can be controlled since the nanoparticles bound to a cell surface are taken up into the cell with time.

公开(公告)号：US09415060B2

公开(公告)日：2016-08-16

申请号：US14340845

申请日：2014-07-25

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Kwang Meyung Kim ,  Sun Hwa Kim ,  Ick Chan Kwon ,  Ji Young Yhee ,  Sojin Lee

IPC: A61K47/48 ,  A61K31/7088 ,  A61K31/713

CPC classification number: A61K31/7088 ,  A61K31/713 ,  A61K47/6435 ,  A61K47/6903 ,  A61K47/6929

Abstract: Disclosed is a gelatin-based nanoparticle complex for tumor-targeted delivery of siRNA for specific gene silencing in tumor cells. The gelatin-based nanoparticle complex includes: poly-siRNA chains whose ends are modified with thiol groups; and thiolated gelatin bound to the poly-siRNA chains through disulfide crosslinking and charge interactions. The gelatin-based nanoparticle complex is not degraded in the bloodstream and can be efficiently absorbed into tumor cells without cytotoxicity. The delivered siRNA can effectively silence target gene expression. Also disclosed is a method for preparing the gelatin-based nanoparticle complex.

Abstract translation: 公开了一种用于肿瘤靶向递送siRNA用于肿瘤细胞中特异性基因沉默的明胶基纳米颗粒复合物。 基于明胶的纳米颗粒复合物包括：末端用巯基修饰的多siRNA链; 并通过二硫键交联和电荷相互作用将与siRNA结合的多聚siRNA链结合在一起。 基于明胶的纳米颗粒复合物在血液中不降解，并且可以有效地吸收到肿瘤细胞中而没有细胞毒性。 递送的siRNA可以有效地沉默靶基因表达。 还公开了一种制备明胶基纳米颗粒复合物的方法。

公开(公告)号：US09409923B2

公开(公告)日：2016-08-09

申请号：US13936768

申请日：2013-07-08

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

Inventor： Kwang Meyung Kim ,  Ick Chan Kwon ,  Sang Yoon Kim ,  Ju Hee Ryu ,  Eun Sung Jun ,  In San Kim

IPC: C07D499/78 ,  C07D209/62 ,  C07D409/14 ,  C07D498/08

CPC classification number: C07D499/78 ,  C07D209/62 ,  C07D409/14 ,  C07D498/08

Abstract: Disclosed is a drug-fluorophore complex for specific detection of tumor cells. Specifically, the drug-fluorophore complex includes a tumor cell-targeting drug penetrating tumor cells and non-tumor cells at different rates or levels, and a fluorescent substance chemically bonded to the tumor cell-targeting drug. The drug-fluorophore complex enables specific imaging of tumor cells only with high accuracy in a very simple manner without causing cytotoxicity.

Abstract translation: 公开了用于特异性检测肿瘤细胞的药物 - 荧光团复合物。 具体地，药物 - 荧光团复合物包括以不同速率或水平渗透肿瘤细胞和非肿瘤细胞的肿瘤细胞靶向药物和与肿瘤细胞靶向药物化学键合的荧光物质。 药物荧光团复合物能够以非常简单的方式以高精度进行肿瘤细胞的特异性成像，而不引起细胞毒性。