公开(公告)号：US09833464B2

公开(公告)日：2017-12-05

申请号：US13519821

申请日：2010-12-29

申请人： In San Kim ,  Byung Heon Lee ,  Maggie J M Lu ,  Hsiang-Fa Liang ,  Yi-ju Ko ,  Ya-Chin Lo ,  Li-Wen Chang ,  Ming-Cheng Wei

发明人： In San Kim ,  Byung Heon Lee ,  Maggie J M Lu ,  Hsiang-Fa Liang ,  Yi-ju Ko ,  Ya-Chin Lo ,  Li-Wen Chang ,  Ming-Cheng Wei

IPC分类号： A61K31/70 ,  A61K31/704 ,  A61K47/48 ,  A61K9/127 ,  A61K38/00

CPC分类号： A61K31/704 ,  A61K9/1271 ,  A61K38/00 ,  A61K47/6911

摘要： The present invention relates to a target-aiming drug delivery system for diagnosis and treatment of cancer containing liposome labeled with peptides which specifically targets interleukin-4 receptors, and a manufacturing method thereof. The liposome which contains anticancer drugs labeled with IL4RPep peptides prepared in accordance with the present invention can deliver drugs to cancer cells in which IL-4 receptors are overexpressed by IL4RPep peptides which specifically bind to IL-4 receptors, and the drug delivery can recognize cancer cells specifically by a label. Thus, IL4RPep peptides can increase the effect of drugs only on cancer tissues and at the same time significantly reduce the side effects on normal tissues, which makes possible in vivo(molecular) imaging and early diagnosis of tumors. Therefore, the liposome which contains anticancer drugs labeled with IL4Pep peptides of the present invention can be applied, as the target-aiming drug delivery system, effectively to the diagnosis and treatment of cancers.

公开(公告)号：US20120294931A1

公开(公告)日：2012-11-22

申请号：US13519821

申请日：2010-12-29

申请人： In San Kim ,  Byung Heon Lee ,  Maggie JM Lu ,  Hsiang-Fa Liang ,  Yi-ju Ko ,  Ya-Chin Lo ,  Li-Wen Chang ,  Ming-Cheng Wei

发明人： In San Kim ,  Byung Heon Lee ,  Maggie JM Lu ,  Hsiang-Fa Liang ,  Yi-ju Ko ,  Ya-Chin Lo ,  Li-Wen Chang ,  Ming-Cheng Wei

IPC分类号： A61K9/127 ,  A61P35/00 ,  A61K31/704

CPC分类号： A61K31/704 ,  A61K9/1271 ,  A61K38/00 ,  A61K47/6911

摘要： The present invention relates to a target-aiming drug delivery system for diagnosis and treatment of cancer containing liposome labeled with peptides which specifically targets interleukin-4 receptors, and a manufacturing method thereof. The liposome which contains anticancer drugs labeled with IL4RPep peptides prepared in accordance with the present invention can deliver drugs to cancer cells in which IL-4 receptors are overexpressed by IL4RPep peptides which specifically bind to IL-4 receptors, and the drug delivery can recognize cancer cells specifically by a label. Thus, IL4RPep peptides can increase the effect of drugs only on cancer tissues and at the same time significantly reduce the side effects on normal tissues, which makes possible in vivo(molecular) imaging and early diagnosis of tumors. Therefore, the liposome which contains anticancer drugs labeled with IL4Pep peptides of the present invention can be applied, as the target-aiming drug delivery system, effectively to the diagnosis and treatment of cancers.

摘要翻译： 本发明涉及用于诊断和治疗特异性靶向白介素-4受体的肽标记的含有脂质体的癌症靶向药物递送系统及其制造方法。 含有根据本发明制备的用IL4RPep肽标记的抗癌药物的脂质体可将药物递送至IL-4受体被特异性结合IL-4受体的IL4Rep肽过表​​达的癌细胞，并且药物递送可以识别癌症 细胞特异性地通过标记。 因此，IL4RPep肽可以增加药物对癌症组织的影响，同时显着降低对正常组织的副作用，这使得体内（分子）成像和肿瘤早期诊断成为可能。 因此，含有本发明的IL4Pep肽标记的抗癌药物的脂质体可以作为靶向药物递送系统有效地应用于癌症的诊断和治疗。

公开(公告)号：US20090074663A1

公开(公告)日：2009-03-19

申请号：US12009359

申请日：2008-01-18

申请人： Byung Heon Lee ,  In San Kim ,  Hai Yan Hong ,  In Seop So

发明人： Byung Heon Lee ,  In San Kim ,  Hai Yan Hong ,  In Seop So

IPC分类号： A61K51/00 ,  C07K7/00 ,  C12N15/11 ,  C12N15/00 ,  A61P9/00 ,  A61K38/00 ,  C12N5/06 ,  A61K49/00

CPC分类号： G01N33/6893 ,  C07K7/06 ,  G01N2800/323

摘要： A peptide for diagnosing, preventing and treating atherosclerosis, and a use thereof, comprising an amino acid sequence as set forth in SEQ ID NO: 1 or SEQ ID NO: 2, and a use thereof. The peptide effectively targets atherosclerotic plaques, and binds to IL-4R to thereby exhibit antagonistic effects on IL-4-mediated signaling of cellular inflammatory reaction and survival reaction. The peptide of the present invention can be used for diagnosis of atherosclerosis, prevention and treatment of IL-4-induced inflammatory reaction and prevention and treatment of atherosclerosis which is primarily caused by the inflammatory reaction, as well as for prevention or treatment of atherosclerosis via conjugation with an anti-atherosclerotic drug.

摘要翻译： 用于诊断，预防和治疗动脉粥样硬化的肽及其用途，其包含SEQ ID NO：1或SEQ ID NO：2所示的氨基酸序列及其用途。 该肽有效靶向动脉粥样硬化斑块，并结合IL-4R，从而对IL-4介导的细胞炎症反应和存活反应的信号传导具有拮抗作用。 本发明的肽可用于诊断动脉粥样硬化，预防和治疗IL-4诱导的炎性反应以及主要由炎性反应引起的动脉粥样硬化的预防和治疗，以及预防或治疗动脉粥样硬化通过 与抗动脉粥样硬化药物结合。

公开(公告)号：US20090285754A1

公开(公告)日：2009-11-19

申请号：US12465007

申请日：2009-05-13

申请人： Byung Heon Lee ,  In San Kim

发明人： Byung Heon Lee ,  In San Kim

IPC分类号： A61K51/00 ,  C07K7/06 ,  C07H21/04 ,  C12N15/63 ,  C12N5/00 ,  G01N33/53 ,  A61K38/08 ,  A61K49/00

CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/64 ,  A61K49/0032 ,  A61K49/0043 ,  A61K49/0056 ,  C07K2319/33 ,  G01N2510/00

摘要： The present invention relates to a peptide capable of specifically targeting apoptotic cells undergoing apoptosis and a use thereof. More particularly, it relates to a peptide having an amino acid sequence represented by anyone selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 12 and targeting apoptotic cells, a composition for detection of apoptotic cells comprising the same as an effective ingredient, a composition for drug delivery comprising the same as an effective ingredient, a composition for imaging comprising the same as an effective ingredient and the like. The peptide of the present invention effectively detects apoptosis which is involved in tissues of neoplastic disease, myocardial infarction, stroke and arteriosclerosis. Accordingly, the peptide of the present invention may be used in imaging of diagnosis of the said diseases and reaction against a drug by binding imaging reagent and etc. as well as in protection and treatment for the said diseases by binding a treatment reagent and then delivering drug selectively.

摘要翻译： 本发明涉及能够特异性靶向经历凋亡的凋亡细胞的肽及其用途。 更具体地说，本发明涉及一种具有由选自SEQ ID NO：1至SEQ ID NO：12的任何一个所代表的氨基酸序列并且靶向凋亡细胞的肽，用于检测凋亡细胞的组合物包含与SEQ ID NO： 有效成分，用于药物递送的组合物，其包含与有效成分相同的组合物，用于成像的组合物，其包含其作为有效成分等。 本发明的肽有效地检测参与肿瘤性疾病，心肌梗死，中风和动脉硬化的组织的凋亡。 因此，本发明的肽可以用于诊断所述疾病的成像和通过结合成像试剂等对药物的反应，以及通过结合治疗试剂来保护和治疗所述疾病，然后递送 药物选择性。

公开(公告)号：US20120316101A1

公开(公告)日：2012-12-13

申请号：US13467689

申请日：2012-05-09

申请人： Byung Heon Lee ,  In San Kim

发明人： Byung Heon Lee ,  In San Kim

IPC分类号： C07K7/06 ,  A61K38/08 ,  A61P35/00 ,  A61P9/10 ,  A61P35/02 ,  G01N27/72 ,  C12N1/21 ,  C12N9/96 ,  G01N21/64 ,  G01N21/78 ,  G01N21/25 ,  C12N15/11 ,  A61P25/00

CPC分类号： A61K47/48246 ,  A61K38/00 ,  A61K47/64 ,  A61K49/0032 ,  A61K49/0043 ,  A61K49/0056 ,  C07K7/06 ,  C07K2319/33 ,  G01N2510/00

摘要： The present invention relates to a polypeptide capable of specifically targeting apoptotic cells undergoing apoptosis and a use thereof. More particularly, it relates to an isolated polypeptide consisting of the sequence (I): Cys-X1-Val-Ala-Pro-X2 (I), wherein X1 is an amino acid with polar uncharged side chain and X2 is an amino acid with positive charged side chain and targeting apoptotic cells, a composition for detection of apoptotic cells comprising the same as an effective ingredient, a composition for drug delivery comprising the same as an effective ingredient, a composition for imaging comprising the same as an effective ingredient and the like. Accordingly, the peptide of the present invention may be useful for detection of apoptotic cells, as well as detection and imaging of apoptotic cells in tumor tissue, apoptotic myocardial cells in myocardial infarction tissue, apoptotic nerve cells in stroke tissue and arteriosclerosis site, and targeted drug delivery thereto.

摘要翻译： 本发明涉及能够特异性靶向经历凋亡的凋亡细胞的多肽及其用途。 更具体地，涉及由序列（I）：Cys-X1-Val-Ala-Pro-X2（I）组成的分离的多肽，其中X1是具有极性不带电侧链的氨基酸，X2是具有 阳性带电侧链和靶向凋亡细胞，用于检测包含其作为有效成分的凋亡细胞的组合物，用于药物递送的组合物，其包含作为有效成分的组合物，用于成像的组合物，其包含作为有效成分的组合物和 喜欢。 因此，本发明的肽可用于检测凋亡细胞，以及肿瘤组织中凋亡细胞，心肌梗死组织中的凋亡性心肌细胞，卒中组织和动脉硬化部位的凋亡性神经细胞的检测和成像以及靶向 给药药物。

公开(公告)号：US08217012B2

公开(公告)日：2012-07-10

申请号：US12465007

申请日：2009-05-13

申请人： Byung Heon Lee ,  In San Kim

发明人： Byung Heon Lee ,  In San Kim

IPC分类号： A61K38/08 ,  A61K49/00 ,  A61K51/00 ,  C07K7/06

CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/64 ,  A61K49/0032 ,  A61K49/0043 ,  A61K49/0056 ,  C07K2319/33 ,  G01N2510/00

摘要： A peptide capable of specifically targeting apoptotic cells undergoing apoptosis and a use thereof is described. Peptides having an amino acid sequence represented by any one of SEQ ID NO: 1 to SEQ ID NO: 12 targeted apoptotic cell. Uses for compositions comprising the peptides include detection of apoptotic cells drug delivery and imaging. The peptide of the present invention effectively detects apoptosis which is involved in tissues of neoplastic disease, myocardial infarction, stroke and arteriosclerosis. Accordingly, the peptide of the present invention may be bound to an imaging or treatment reagent to be used in diagnosis of diseases, imaging of drug reactions, and treatment for diseases by selective drug delivery.

摘要翻译： 描述了能够特异性靶向经历凋亡的凋亡细胞的肽及其用途。 具有由SEQ ID NO：1至SEQ ID NO：12中任一个表示的氨基酸序列的肽靶向凋亡细胞。 包含肽的组合物的用途包括检测凋亡细胞药物递送和成像。 本发明的肽有效地检测参与肿瘤性疾病，心肌梗死，中风和动脉硬化的组织的凋亡。 因此，本发明的肽可以与用于诊断疾病，药物反应成像和通过选择性药物递送治疗疾病的成像或治疗试剂结合。

公开(公告)号：US08993721B2

公开(公告)日：2015-03-31

申请号：US13467689

申请日：2012-05-09

申请人： Byung Heon Lee ,  In San Kim

发明人： Byung Heon Lee ,  In San Kim

IPC分类号： C07K7/06 ,  A61K38/08 ,  A61K47/48 ,  A61K49/00 ,  A61K38/00

CPC分类号： A61K47/48246 ,  A61K38/00 ,  A61K47/64 ,  A61K49/0032 ,  A61K49/0043 ,  A61K49/0056 ,  C07K7/06 ,  C07K2319/33 ,  G01N2510/00

摘要： Described herein is an isolated polypeptide which is capable of specifically targeting apoptotic cells undergoing apoptosis and consists of the sequence (I): Cys-X1-Val-Ala-Pro-X2 (I), wherein X1 is an amino acid with polar uncharged side chain and X2 is an amino acid with positive charged side chain. The isolated polypeptide of the present invention may be useful for detecting apoptotic cells, as well as detecting and imaging apoptotic cells in tumor tissue, apoptotic myocardial cells in myocardial infarction tissue, apoptotic nerve cells in stroke tissue, and arteriosclerosis site; the polypeptide is useful for targeted drug delivery thereto.

摘要翻译： 本文描述了能够特异性靶向经历凋亡的凋亡细胞并由序列（I）：Cys-X1-Val-Ala-Pro-X2（I）组成的分离的多肽，其中X1是具有极性不带电侧的氨基酸 链和X2是具有正带侧链的氨基酸。 本发明的分离的多肽可用于检测凋亡细胞，以及检测和成像肿瘤组织中的凋亡细胞，心肌梗死组织中的凋亡心肌细胞，卒中组织中的凋亡性神经细胞和动脉硬化部位; 该多肽可用于靶向药物递送。

公开(公告)号：US07968081B2

公开(公告)日：2011-06-28

申请号：US12009359

申请日：2008-01-18

申请人： Byung Heon Lee ,  In San Kim ,  Hai Yan Hong ,  In Seop So

发明人： Byung Heon Lee ,  In San Kim ,  Hai Yan Hong ,  In Seop So

IPC分类号： A61K51/00 ,  A61M36/14

CPC分类号： G01N33/6893 ,  C07K7/06 ,  G01N2800/323

摘要： A peptide for diagnosing, preventing and treating atherosclerosis, and a use thereof, comprising an amino acid sequence as set forth in SEQ ID NO: 1 or SEQ ID NO: 2, and a use thereof. The peptide effectively targets atherosclerotic plaques, and binds to IL-4R to thereby exhibit antagonistic effects on IL-4-mediated signaling of cellular inflammatory reaction and survival reaction. The peptide of the present invention can be used for diagnosis of atherosclerosis, prevention and treatment of IL-4-induced inflammatory reaction and prevention and treatment of atherosclerosis which is primarily caused by the inflammatory reaction, as well as for prevention or treatment of atherosclerosis via conjugation with an anti-atherosclerotic drug.

摘要翻译： 用于诊断，预防和治疗动脉粥样硬化的肽及其用途，其包含SEQ ID NO：1或SEQ ID NO：2所示的氨基酸序列及其用途。 该肽有效靶向动脉粥样硬化斑块，并结合IL-4R，从而对IL-4介导的细胞炎症反应和存活反应的信号传导具有拮抗作用。 本发明的肽可用于诊断动脉粥样硬化，预防和治疗IL-4诱导的炎性反应以及主要由炎性反应引起的动脉粥样硬化的预防和治疗，以及预防或治疗动脉粥样硬化通过 与抗动脉粥样硬化药物结合。