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公开(公告)号:KR101863283B1
公开(公告)日:2018-06-29
申请号:KR1020160049805
申请日:2016-04-25
Applicant: 한국과학기술연구원
IPC: G01N33/574 , G01N33/58 , C07K5/10 , C07K7/06 , A61K49/18
CPC classification number: A61K49/0056 , A61K47/555 , A61K49/0032 , A61K49/0052 , C07K5/1016 , C07K5/1019 , C07K9/001 , G01N33/57496 , G01N33/581 , G01N2333/96466
Abstract: 본발명은암세포표적당펩타이드및 이를포함하는조영제키트에관한것으로, 상기당펩타이드는기질펩타이드에아자이드제공당단량체가결합된것으로, 암세포내에서카뎁신 B 효소에의해상기기질펩타이드가특이적으로분해되어아자이드제공당단량체가글라이코엔지니어링(glycoengineering)에의해세포표면으로발현되어이를표적으로조영제가작용할수 있도록한 것이다. 따라서정상세포에서는발현이제한되면서암세포내에서특이적으로발현되고, 특히전이암에서특이적으로발현되며, 세포외로거의분비되지않는카뎁신 B 효소에의해서만세포표면에아자이드가노출되어아자이드특이적인조영제에의해암세포를선택적으로조영하는것이가능하다.
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公开(公告)号:KR101713888B1
公开(公告)日:2017-03-09
申请号:KR1020157033154
申请日:2011-03-02
Applicant: 한국과학기술연구원
IPC: A61K38/08 , A61K31/7042 , A61K31/337 , A61K51/08
CPC classification number: A61K41/0042 , A61K31/704 , A61K38/00 , A61K47/64 , A61N5/062 , A61N5/1001
Abstract: 본발명은아세틸-서열번호 1의펩타이드-링커-항암제로구성되는항암제전구체에관한것으로, 상기항암제전구체는독소루비신과같이산과염기에불안정한항암제를효과적으로전구체로제공함으로써체내투여시에는비활성상태의항암제전구체로독성이없는상태로존재하지만, 체내투여후 방사선치료나 UV 치료후 활성화되는케스페이즈존재하에서활성성분인항암제가표적부위에서효과적으로방출되므로암세포에만선택적으로항암효과를나타낼수 있어치료효과의극대화및 항암치료의부작용을최소화할수 있다.
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或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。
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公开(公告)号:KR101437885B1
公开(公告)日:2014-09-15
申请号:KR1020120137013
申请日:2012-11-29
Applicant: 한국과학기술연구원
CPC classification number: A61K9/127 , C12N15/88 , C12Q1/686 , C12Q2563/159 , C12Q2563/161
Abstract: 본 발명은 유전자를 세포독성 없이 효과적으로 세포 내로 전달하기 위한 유전자 전달체 및 그 제조방법에 관한 것으로서, 더욱 구체적으로는, 중성 리포좀으로 이루어진 외피; 및 상기 외피에 의해서 한정되는 내부 공간에, 주형 DNA와, 상기 주형 DNA를 PCR 반응에 의해서 증폭하기 위한 중합효소, dNTP 및 프라이머를 포함하는 PCR 기반의 유전자 전달체 및 그 제조방법에 관한 것이다.
본 발명에 따르면, 세포독성 없이 유전자 로딩 효율이 향상된 유전자 전달체 및 그 제조방법을 제공할 수 있다.-
公开(公告)号:KR1020130110218A
公开(公告)日:2013-10-08
申请号:KR1020137020823
申请日:2011-03-02
Applicant: 한국과학기술연구원
IPC: A61K38/08 , A61K31/7042 , A61K31/337 , A61K51/08
CPC classification number: A61K41/0042 , A61K31/704 , A61K38/00 , A61K47/64 , A61N5/062 , A61N5/1001
Abstract: PURPOSE: An anticancer agent prodrug is provided to show selective anticancer effects to cancer cells because an anticancer agent which is unstable in acid and base is formed in a prodrug, thereby maximizing cancer treatment effects and minimizing side effects. CONSTITUTION: A prodrug composition contains acetyl, a peptide of sequence number 1, a linker, and an anticancer agent, which are sequentially connected. Acetyl and the peptide are cleaved by activated caspase. An anticancer kit contains: the prodrug composition; and a radiation or UV ray irradiating device which irradiates a subject by radiation or UV rays and activates caspase in tumor cells.
Abstract translation: 目的:提供抗癌剂前药以显示对癌细胞的选择性抗癌作用,因为在前药中形成在酸和碱中不稳定的抗癌剂,从而最大化癌症治疗效果并尽量减少副作用。 构成:前药组合物含有顺序连接的乙酰基,序列号1的肽,接头和抗癌剂。 乙酰基和肽被激活的半胱天冬酶切割。 抗癌试剂盒包含:前药组合物; 以及通过辐射或紫外线照射受试者并在肿瘤细胞中激活半胱天冬酶的辐射或紫外线照射装置。
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公开(公告)号:KR1020120092766A
公开(公告)日:2012-08-22
申请号:KR1020110008258
申请日:2011-01-27
Applicant: 한국과학기술연구원
Abstract: PURPOSE: A nanoparticle containing polymeric derivatives conjugated with peptides is provided to selectively make an image of cell apoptosis in a tissue or cells and to diagnose cancer. CONSTITUTION: An apoptosis-specific nanoparticle contrast agent contains a peptide conjugated with a polymer, a quencher, and a fluorescence substance. The peptide contains a residue which is selectively cleaved by caspase. The polymer is selected among chitosan, glycol chitosan, protamine, polylyscine, polyarginine, polyethylene imine polymer and derivative thereof, dextran, hyalruonic acid, and albumin derivatives. The peptide is specifically cleaved by caspase. An anticancer agent contains the nanoparticle contrast agent.
Abstract translation: 目的:提供含有与肽缀合的聚合衍生物的纳米颗粒,以选择性地在组织或细胞中形成细胞凋亡的图像并诊断癌症。 构成:凋亡特异性纳米颗粒造影剂含有与聚合物,猝灭剂和荧光物质缀合的肽。 肽含有被胱天蛋白酶选择性切割的残基。 聚合物选自壳聚糖,乙二醇壳聚糖,鱼精蛋白,聚赖氨酸,聚精氨酸,聚乙烯亚胺聚合物及其衍生物,葡聚糖,透明质酸和白蛋白衍生物。 肽被半胱天冬酶特异性切割。 抗癌剂含有纳米颗粒造影剂。
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公开(公告)号:KR102239752B1
公开(公告)日:2021-04-13
申请号:KR1020190164258
申请日:2019-12-11
Applicant: 한국과학기술연구원
Abstract: 본발명은서열번호 1로표시되는양친매성펩타이드의일 말단에항암제가결합된약물복합체및 폴록사머를포함하는제1 약학성분; 및항-PD-L1 항체를포함하는제2 약학성분;을유효성분으로포함하는암 예방또는치료를위한병용투여용약학조성물에관한것으로, 생체내 실험을통해암의성장을유의하게억제하였고, 암조직내에서면역세포활성화를통해면역치료의효능을크게증가시키는효과를갖는다. 특히, 본발명에따른병용투여용약학조성물은종래항암제대비우수한종양축적효율및 선택성을가지므로, 암조직을제외한정상조직에대해서는독성을거의나타내지않아매우안정적이다.
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公开(公告)号:KR1020150135796A
公开(公告)日:2015-12-03
申请号:KR1020157033154
申请日:2011-03-02
Applicant: 한국과학기술연구원
IPC: A61K38/08 , A61K31/7042 , A61K31/337 , A61K51/08
CPC classification number: A61K41/0042 , A61K31/704 , A61K38/00 , A61K47/64 , A61N5/062 , A61N5/1001
Abstract: 본발명은아세틸-서열번호 1의펩타이드-링커-항암제로구성되는항암제전구체에관한것으로, 상기항암제전구체는독소루비신과같이산과염기에불안정한항암제를효과적으로전구체로제공함으로써체내투여시에는비활성상태의항암제전구체로독성이없는상태로존재하지만, 체내투여후 방사선치료나 UV 치료후 활성화되는케스페이즈존재하에서활성성분인항암제가표적부위에서효과적으로방출되므로암세포에만선택적으로항암효과를나타낼수 있어치료효과의극대화및 항암치료의부작용을최소화할수 있다.
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或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。
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公开(公告)号:KR1020140046704A
公开(公告)日:2014-04-21
申请号:KR1020120112522
申请日:2012-10-10
Applicant: 한국과학기술연구원
CPC classification number: A61K49/0056 , A61K38/1808 , A61K47/18 , A61K47/20 , A61K47/66 , A61K49/0032
Abstract: The present invention relates to an epidermal growth factor receptor (EGFR)-positive tumor targeted quenched nanoprobe and to a method of producing same and, more particularly, to an EGFR-positive tumor targeted quenched nanoprobe, wherein a fluorescent body and a quenching body are conjugated to an epidermal growth factor (EGF), and to a method of producing the same. The EGFR-positive tumor targeted quenched nanoprobe (EGF-NP) can specifically detect the EGFR-positive tumor and accordingly can effectively monitor the therapeutic effects of EGFR-targeted drugs. Moreover, imaging is performed in a short time so that repeated image acquisition can be performed easily and simply and continuous image data over time can be effectively obtained. Furthermore, the EGF-NP according to the present invention has excellent stability in the human body as the EGF-NP dissipates in the human body after a period of time. [Reference numerals] (AA) Quenching body; (BB) Quenched fluorescent body; (CC) Active fluorescent body; (DD) Tumor cell; (EE) Targeted bond for EGFR on the tumor cell; (FF) Inject inside and decompose lysosomes
Abstract translation: 本发明涉及表皮生长因子受体(EGFR)阳性肿瘤靶向淬灭的纳米探针及其制备方法,更具体地涉及EGFR阳性肿瘤靶向淬灭的纳米探针,其中荧光体和淬火体为 与表皮生长因子(EGF)缀合的方法及其制备方法。 EGFR阳性肿瘤靶向淬灭纳米探针(EGF-NP)可以特异性检测EGFR阳性肿瘤,从而有效监测EGFR靶向药物的治疗效果。 此外,在短时间内执行成像,使得可以容易且简单地执行重复的图像采集,并且可以有效地获得随时间的连续的图像数据。 此外,根据本发明的EGF-NP在一段时间后在人体内消散的EGF-NP在人体中具有优异的稳定性。 (标号)(AA)淬火体; (BB)淬火荧光体; (CC)活性荧光体; (DD)肿瘤细胞; (EE)肿瘤细胞上EGFR靶向键; (FF)注入内部并分解溶酶体
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