Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 7, Pages 1453-1462Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.02.014
Keywords
Pheophorbide-a; Conjugate; Fluorescence; Apoptosis; PDT
Funding
- Ministry of Health & Welfare, Republic of Korea [A100490]
- National Research Foundation of Korea (NRF) - Ministry of Science, ICT & Future Planning [NRF-2014R1A2A1A11052300]
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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 alpha(v)beta(6) 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 alpha(v)beta(6) receptor. (C) 2015 Elsevier Ltd. All rights reserved.
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