CHOI, YONG DOOKR,최용두,KIM, JI SUKR,김지수,KIM, HYUN JINKR,김현진,LEE, HA WONKR,이하원
申请号：
KR1020140054923
公开号：
KR1020150128103A
申请日:
2014.05.08
申请国别(地区):
KR
年份:
2015
代理人:
摘要：
The present invention relates to a conjugate for photodynamic diagnosis or therapy, in which folic acid is conjugated to a photosensitizer or a near-infrared fluorescent dye through an intracellularly cleavable link, and to a composition for photodynamic diagnosis or therapy containing the same. In the present invention, the folic acid functions as a target ligand for cells overexpressing a folic acid receptor, and also plays a role in extinction of optical properties of the fluorescent dye and the photosensitizer. In the case of forming the conjugate of folic acid and the fluorescent dye or the photosensitizer through a cleavable linker of 0.5 to 10 nm in length, a fluorescent signal and reactive oxygen are not generated by the extinction by folic acid. After the conjugate is specifically taken into the cells overexpressing the folic acid receptor, and the linker of the conjugate is cleaved by an endoenzyme, a reducing agent, or a low pH so the folic acid becomes distant from the fluorescent dye or the photosensitizer, the folic acid cannot act as a quencher anymore so that a strong fluorescent signal can be generated and an effect of photodynamic therapy also appears. The conjugate for photodynamic diagnosis or therapy containing folic acid in accordance with the present invention has high tissue permeability, is safe for normal cells but has a strong therapeutic effect only in target cells (for example, cancer cells), and can obtain a good diagnostic image with a high signal rate compared to background by an extinction function of the folic acid.COPYRIGHT KIPO 2016본 발명은 엽산이 세포내 분해 가능한 연결을 통해 광증감제 또는 근적외선 형광염료와 결합된 광역학 진단 또는 치료용 결합체 및 이를 포함하는 광역학 진단 또는 치료용 조성물에 관한 것이다. 본 발명에서 엽산은 엽산 수용체를 과발현 하는 세포에 대한 표적 리간드로서의 기능뿐만 아니라, 형광염료 및 광증감제의 광학 특성을 소광시키는 작용을 하고 있다. 0.5nm ~ 10nm 길이의 분해 가능한 연결자를 통하여 엽산과 형광염료 또는 광증감제의 결합체를 형성하는 경우에는, 엽산의 소광작용에 의하여 형광염료 및 광증감제로부터 형광신호와 반응성 산소가 발생하지 않는다. 결합체가 엽산 수용체를 과발현 하는 세포내로 특이적으로 섭취되고 세포내 효소, 환원제, 또는 낮은 pH 환경에 의해서 결합체의 연결자가 분해되고 엽산과 형광염료
