Title:
CONJUGATE FOR PHOTODYNAMIC DIAGNOSIS OR THERAPY, CONTAINING FOLIC ACID, AND COMPOSITION FOR PHOTODYNAMIC DIAGNOSIS OR THERAPY, CONTAINING SAME
Document Type and Number:
WIPO Patent Application WO/2015/170878
Kind Code:
A1
Abstract:
The present invention relates to: a conjugate for photodynamic diagnosis or therapy, in which folic acid is coupled to a photosensitizer or a near-infrared fluorescent dye through an intracellular cleavable link; and a composition for photodynamic diagnosis or therapy, containing the same. In the present invention, folic acid functions as a target ligand for cells, overexpressing a folic acid receptor, and quenches the optical properties of a fluorescent dye and a photosensitizer. A fluorescent signal and reactive oxygen are not generated from a fluorescent dye and a photosensitizer by the quenching action of folic acid when a conjugate of folic acid and a fluorescent dye or a photosensitizer is formed through a cleavable linker having a length of 0.5-10 nm. Folic acid can no longer function as a quencher after the conjugate is specifically taken into cells overexpressing a folic acid receptor, a linker of the conjugate is decomposed by an endoenzyme, a reducing agent or a low pH environment, and the distance between folic acid and a fluorescent dye or a photosensitizer increases, and thus a strong fluorescent signal can be generated and photodynamic therapy effects are also exhibited from this point on. The conjugate for photodynamic diagnosis or therapy, containing folic acid, according to the present invention has high tissue permeability, is safe in normal cells but exhibits high treatment effects only in target cells (for example, cancer cells), and allows a good diagnostic image having a high signal-to-background ratio to be obtained through the quenching function of folic acid.
Inventors:
CHOI YONG-DOO (KR)
KIM JI-SU (KR)
KIM HYUN-JIN (KR)
LEE HA-WON (KR)
KIM JI-SU (KR)
KIM HYUN-JIN (KR)
LEE HA-WON (KR)
Application Number:
PCT/KR2015/004528
Publication Date:
November 12, 2015
Filing Date:
May 07, 2015
Export Citation:
Assignee:
NAT CANCER CT (KR)
International Classes:
C07D239/70; A61K31/519; A61K31/538; A61K47/48; A61K49/10
Foreign References:
| KR20110038215A | 2011-04-14 | |||
| KR20110101338A | 2011-09-16 |
Other References:
YANG, J. ET AL.: "Evaluation of disulfide reduction during receptor-mediated endocytosis by using FRET imaging", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 103, no. 37, 2006, pages 13872 - 13877, XP002519657, ISSN: 0027-8424
SCHNEIDER, R. ET AL.: "Design, synthesis, and biological evaluation of folic acid targeted tetraphenylporphyrin as novel photosensitizers for selective photodynamic therapy", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 13, no. 8, 2005, pages 2799 - 2808, XP027637588, ISSN: 0968-0896
SCHNEIDER, R. ET AL.: "Design, synthesis, and biological evaluation of folic acid targeted tetraphenylporphyrin as novel photosensitizers for selective photodynamic therapy", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 13, no. 8, 2005, pages 2799 - 2808, XP027637588, ISSN: 0968-0896
Attorney, Agent or Firm:
WIE, Byoung-Gap (KR)
위병갑 (KR)
위병갑 (KR)
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