公开(公告)号：US09408911B2

公开(公告)日：2016-08-09

申请号：US14974490

申请日：2015-12-18

Applicant: Korea Institute of Science and Technology

Inventor： Ju-Hee Ryu ,  Kwang-Meyung Kim ,  Ick-Chan Kwon ,  Kui-Won Choi ,  Sang-Yoon Kim ,  Beom-Suk Lee ,  Dae-Yoon Chi ,  Hee-Seup Kil ,  Hyun-Ju Sung

IPC: A61K41/00 ,  A61N5/06 ,  A61N5/10

CPC classification number: A61K41/0042 ,  A61K31/704 ,  A61K38/00 ,  A61K47/64 ,  A61N5/062 ,  A61N5/1001

Abstract: The present invention relates to an anticancer prodrug consisting of peptide of acetyl-SEQ ID NO: 1-linker-anticancer drug. The anticancer prodrug effectively provides an anticancer drug unstable in acid and base, such as doxorubicin, in a form of prodrug. Thus, the anticancer prodrug exists as a non-toxic inactive form when administered into the body, but effectively releases the anticancer drug as an active ingredient in the target area in the presence of caspase activated by radiation or UV treatment after administered into the body. Accordingly, the anticancer drug exhibits selective anticancer effects on cancer cells, thereby maximizing the therapeutic effect and minimizing the side-effects of chemotherapy.

Abstract translation: 本发明涉及一种由乙酰基-SEQ ID NO.1-接头 - 抗癌药物的肽组成的抗癌药物。 抗癌前药有效地提供了在酸和碱中不稳定的抗癌药物，例如以前药形式的多柔比星。 因此，当施用于体内时，抗癌前药以无毒无活性形式存在，但在施用于体内后，通过辐射或UV治疗活化的半胱天冬酶存在下，有效地将抗癌药物作为活性成分释放到目标区域。 因此，抗癌药物对癌细胞具有选择性的抗癌作用，从而最大化治疗效果并使化疗的副作用最小化。

公开(公告)号：US20160184430A1

公开(公告)日：2016-06-30

申请号：US14974490

申请日：2015-12-18

Applicant: Korea Institute of Science and Technology

Inventor： Ju-Hee Ryu ,  Kwang-Meyung Kim ,  Ick-Chan Kwon ,  Kui-Won Choi ,  Sang-Yoon Kim ,  Beom-Suk Lee ,  Dae-Yoon Chi ,  Hee-Seup Kil ,  Hyun-Ju Sung

IPC: A61K41/00 ,  A61N5/06 ,  A61K47/48 ,  A61N5/10 ,  A61K9/00 ,  A61K31/704

CPC classification number: A61K41/0042 ,  A61K31/704 ,  A61K38/00 ,  A61K47/64 ,  A61N5/062 ,  A61N5/1001

Abstract: The present invention relates to an anticancer prodrug consisting of peptide of acetyl-SEQ ID NO: 1-linker-anticancer drug. The anticancer prodrug effectively provides an anticancer drug unstable in acid and base, such as doxorubicin, in a form of prodrug. Thus, the anticancer prodrug exists as a non-toxic inactive form when administered into the body, but effectively releases the anticancer drug as an active ingredient in the target area in the presence of caspase activated by radiation or UV treatment after administered into the body. Accordingly, the anticancer drug exhibits selective anticancer effects on cancer cells, thereby maximizing the therapeutic effect and minimizing the side-effects of chemotherapy.

Abstract translation: 本发明涉及一种由乙酰基-SEQ ID NO.1-接头 - 抗癌药物的肽组成的抗癌药物。 抗癌前药有效地提供了在酸和碱中不稳定的抗癌药物，例如以前药形式的多柔比星。 因此，当施用于体内时，抗癌前药以无毒无活性形式存在，但在施用于体内后，通过辐射或UV治疗活化的半胱天冬酶存在下，有效地将抗癌药物作为活性成分释放到目标区域。 因此，抗癌药物对癌细胞具有选择性的抗癌作用，从而最大化治疗效果并使化疗的副作用最小化。

公开(公告)号：US08889647B2

公开(公告)日：2014-11-18

申请号：US13742901

申请日：2013-01-16

Applicant: Korea Institute of Science and Technology

Inventor： Hyung-Jun Ahn ,  Ick-Chan Kwon ,  Kui-Won Choi

IPC: C07H21/04 ,  C07K14/00

CPC classification number: C07K14/001 ,  A61K47/62 ,  C07K14/08 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/32

Abstract: Recombinant proteins for siRNA delivery and a composition including same. These recombinant proteins include a p19 RNA binding protein and a target oriented peptide and can secure the stability of siRNAs from external attacks such as various degradation enzymes, have selective binding affinity to cancer cells by virtue of target-oriented peptides having various cancer cells as their target, and silence target genes by effectively delivering the siRNAs to cells and biological tissues by the release of the siRNAs to the cytoplasms after the cell penetration thereof. Therefore, they are expected to be effectively employed as siRNA delivery vehicles for siRNA therapeutic agents, cell-based drug screening compositions and research.

Abstract translation: 用于siRNA递送的重组蛋白质和包含其的组合物。 这些重组蛋白包括p19 RNA结合蛋白和靶向肽，并且可以确保siRNA从诸如各种降解酶的外部攻击的稳定性，由于具有各种癌细胞的靶向肽具有与癌细胞的选择性结合亲和力 目标和沉默靶基因，通过在siRNA细胞穿透细胞后将siRNA释放到细胞质中，将siRNA有效递送至细胞和生物组织。 因此，预期它们将有效地用作siRNA治疗剂，基于细胞的药物筛选组合物和研究的siRNA递送载体。