title: Pheophorbide-a conjugates with cancer-targeting moieties for targeted photodynamic cancer therapy.
abstract: Pheophorbide-a, a non-selective photosensitizer, was conjugated with cancer-targeting moieties, such as folic acid, the CRGDLASLC peptide, the cRGDfK peptide and leuprorelin, for the purpose of targeted photodynamic cancer therapy. The cellular uptake of pheophorbide-a conjugates in cancer cells overexpressing the corresponding receptors of the targeting moieties was largely enhanced compared with that in the receptor-negative cells. In the study of in vitro photodynamic activity and selectivity of pheophorbide-a conjugates in the receptor-positive and receptor-negative cells, a pheophorbide-a conjugate, (14) with an αvβ6 ligand (CRGDLASLC) exhibited the highest selectivity in the positive FaDu cells. Targeted PDT with 14 induced cell death through apoptosis and morphological apoptosis-like characteristics. These results suggest that pheophorbide-a conjugate 14 could be utilized in selective photodynamic therapy for oral cancers primarily expressing the αvβ6 receptor.
authors.affiliation: Department of Medical System Engineering (DMSE), Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju 500-712, Republic of Korea.
authors.forename: Hyun
authors.initials: H
authors.lastname: You
authors.affiliation: Department of Oral & Maxillofacial Pathology, College of Dentistry, Deajeon Dental Hospital, Wonkang University, 77, Dunsan-ro, Seo-gu, Daejeon 302-120, Republic of Korea.
authors.forename: Hyo-Eun
authors.initials: HE
authors.lastname: Yoon
authors.affiliation: Department of Medical System Engineering (DMSE), Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju 500-712, Republic of Korea.
authors.forename: Pyeong-Hwa
authors.initials: PH
authors.lastname: Jeong
authors.affiliation: School of Life Science, Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju 500-712, Republic of Korea. Electronic address: kohyojin@gist.ac.kr.
authors.forename: Hyojin
authors.initials: H
authors.lastname: Ko
authors.affiliation: Department of Oral & Maxillofacial Pathology, College of Dentistry, Deajeon Dental Hospital, Wonkang University, 77, Dunsan-ro, Seo-gu, Daejeon 302-120, Republic of Korea. Electronic address: opath@wku.ac.kr.
authors.forename: Jung-Hoon
authors.initials: JH
authors.lastname: Yoon
authors.affiliation: Department of Medical System Engineering (DMSE), Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju 500-712, Republic of Korea; School of Life Science, Gwangju Institute of Science and Technology, 123 Cheomdangwagi-ro, Buk-gu, Gwangju 500-712, Republic of Korea. Electronic address: yongchul@gist.ac.kr.
authors.forename: Yong-Chul
authors.initials: YC
authors.lastname: Kim
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002734:Chlorophyll / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D017319:Photosensitizing Agents; D002734:Chlorophyll; C032623:pheophorbide a
keywords: Apoptosis; Conjugate; Fluorescence; PDT; Pheophorbide-a