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Published in Kitsakorn Locharoenrat, Research Methodologies for Beginners, 2017
Many metal-free organic dyes showed promising results in photovoltaic application. Those are derivatives of coumarin, triphenylamine, carbazole, and indoline [2,4,6]. Coumarin-153 is a derivative of coumarin, with additional electron-donor and electron-acceptor groups. Electron-donor group greatly lowers the energy of and . In addition electron-acceptor group is as well shifting fluorescence and absorption maximum peak to longer wavelengths, resulting in absorption peak of coumarin-153 at 430 nm, compared to 365 nm for coumarin [7]. For that reason, goal of this work is to efficiently combine ZnO, which is very commonly used material for solar cells because of its optical properties, with coumarin-153, which reported promising results in photovoltaic application with TiO2, in order to enhance efficiency of ZnO sunlight absorption [7–9].
Novel approaches to targeted protein degradation technologies in drug discovery
Published in Expert Opinion on Drug Discovery, 2023
Yu Xue, Andrew A. Bolinger, Jia Zhou
Taking advantage of the overexpression of nitroreductase (NTR) in hypoxic cells, Zhu’s group designed an NTR-responsive Pre-PROTAC 48, by incorporating a nitroimidazole caging group on VHL ligand [65]. The caging group was recognized by NTR for cleavage, thereby releasing active 48 to efficiently degrade EGFR and subsequently exert antitumor efficacy. Chen’s group reported several caged ROS-responsive PROTACs using arylboronic acid as the caging group [66]. The authors investigated the attaching sites on the glutarimide or amine of CRBN ligand and found that the latter was superior to caging group cleavage when treated with H2O2. Finally, Pre-PROTAC 49 efficiently degraded BRD3 and selectively inhibited the proliferation of T47D cells with higher ROS levels. He’s group recently reported a novel approach that applied light and ROS levels as cascading triggers [67]. By conjugating photosensitizers (PS) to POI ligands, they constructed PS-Degrons that can produce cytotoxic singlet oxygen by visible light, thereby causing unspecific oxidative damage to POI and subsequently recruiting UPS for degradation. The most potent PS-Degron, PSDalpha (50), was synthesized by conjugating triphenylamine benzothiadiazole (PS part) and 17β-estradiol (POI ligand) via an acetylene bond, and it completely degraded estrogen receptor α (ERα) to achieve an excellent anti-proliferative activity in MCF-7 cells.