Korea Institute of Science and Technology

The Asan Foundation

Futurechem Co., Ltd

Kwang-Meyung Kim

Ick-Chan Kwon

Kui-Won Choi

Kyeong-Soon Park

Dae-Yoon Chi

In-Chan Youn

Seul-Ki Lee

Sang-Yoon Kim

Hyun-Ju Sung

Hee-Seup Kil

Ju-Hee Ryu

Beom-Suk Lee

Jong-Ho Kim

Seung-Jin Lee

Cheol-hee Ahn

Seung-Jae Myung

Dae-hyuk Moon

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 or 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.

Anticancer prodrug activated by radiation or ultraviolet treatment and use thereof

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.

Anticancer prodrugs activated by radiation or ultraviolet treatment and use thereof

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.

Nanoparticle sensor for measuring protease activity and method for manufacturing the same

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.

Photosensitizer based on polymer derivatives-photosensitizer conjugates for photodynamic therapy

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.

Gold nanoparticle based protease imaging probes and use thereof

Disclosed are Ionic complex nanoparticles for detecting heparanase activities and a method for preparing the same. More specifically, disclosed are Ionic complex nanoparticles for detecting heparanase activities, wherein negative-ion substrate polymers specifically degraded by heparanase and positive-ion biocompatible polymers ionically bind to each other, and fluorophores or quenchers bind to each of the polymers. The ionic complex nanoparticles for detecting heparanase activities may be applied to a method for screening novel drugs such as inhibitors that prevent over-expression of heparanase. Various cells and tissues where over-expression of heparanase occurs may be non-invasively imaged in cancer cells, cancer tissues, and tissues of various inflammatory diseases. Accordingly, the ionic complex nanoparticles for detecting heparanase activities may be effectively used to early diagnose various diseases and incurable diseases including autoimmune diseases such as cancers, osteoarthritis, rheumatoid arthritis, and dementia.

Ionic complex nanoparticles for detecting heparanase activities and method for preparing the same

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Seoul, South Korea

Kwang-Meyung Kim