Publication: Resorufin enters the photodynamic therapy arena: a monoamine oxidase activatable agent for selective cytotoxicity
Program
KU Authors
Co-Authors
Atakan, Gizem
Gunbas, Gorkem
Advisor
Publication Date
2020
Language
English
Type
Journal Article
Journal Title
Journal ISSN
Volume Title
Abstract
A red-absorbing, water-soluble, and iodinated resorufin derivative (R1) that can be selectively activated with a monoamine oxidase (MAO) enzyme was synthesized, and its potential as a photodynamic therapy (PDT) agent was evaluated. R1 showed high O-1(2) generation yields in aqueous solutions upon addition of MAO isoforms, and it was further tested in cell culture studies. R1 induced photocytotoxicity after being triggered by endogenous MAO enzyme in cancer cells with a much higher efficiency in SH-SYSY neuroblastoma cells with high MAO-A expression. Additionally, R1 displayed differential cytotoxicity between cancer and normal cells, without any considerable dark toxicity. To the best of our knowledge, R1 marks the first example of a resorufin-based photosensitizer (PS) as well as the first anticancer drug that is activated by a MAO enzyme. Remarkably, the target PDT agent was obtained only in three steps as a result of versatile resorufin chemistry.
Description
Source:
Acs Medicinal Chemistry Letters
Publisher:
Amer Chemical Soc
Keywords:
Subject
Chemistry, Medicinal