Design and synthesis of a luminescent iridium complex-peptide hybrid (IPH) that detects cancer cells and induces their apoptosis.

@article{Masum2018DesignAS,
  title={Design and synthesis of a luminescent iridium complex-peptide hybrid (IPH) that detects cancer cells and induces their apoptosis.},
  author={Abdullah Al Masum and Kenta Yokoi and Yosuke Hisamatsu and Kana Naito and Babita Shashni and Shin Aoki},
  journal={Bioorganic \& medicinal chemistry},
  year={2018},
  volume={26 17},
  pages={
          4804-4816
        }
}
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TLDR
The design and synthesis of C 3-symmetric and luminescent Ir complex-peptide hybrids (IPHs) are reported on, which possess cyclic peptide that had been reported to bind DR5 and induce slow cell death of these cancer cells in a parallel manner to the DR5 expression level.
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TLDR
It is found that xestospongin C, a selective inhibitor of an inositol 1,4,5-trisphosphate receptor located on the endoplasmic reticulum (ER), reduces the cytotoxicity of 2c, suggesting that 2c triggers the release of Ca2+ from the ER, leading to an increase in the concentration of cytosolic Ca2+, thus inducing cell death.
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TLDR
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Membrane localized iridium(III) complex induces endoplasmic reticulum stress and mitochondria-mediated apoptosis in human cancer cells.
TLDR
A series of novel luminescent cationic iridium(III) complexes are synthesized by tuning the ancillary N(∧)N ligand based on a structure [Ir(ppy)2(N(∩)N)](+), with 3 exhibiting the highest cellular uptake efficiency and the greatest cytotoxic activities in several cancer cell lines with IC50s lower than that of cisplatin.
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TLDR
The design and synthesis of a new pH-sensitive cyclometalated Ir(III) complex containing a 2-(5'-N,N-diethylamino-4'-tolyl)pyridine (deatpy) ligand is reported on, which exhibits a considerable change in emission intensity between neutral and slightly acidic pH.
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TLDR
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TLDR
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TLDR
Novel reaction-based nuclear staining for visualizing exclusively the nuclei of living cells with a significant luminescence enhancement may extend the arsenal of currently available fluorescent stains for specific staining of cellular compartments.
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TLDR
The data support the notion that inter-ligand distance, relative spatial orientation and copy number of receptor-binding modules are key prerequisites for receptor activation and cell killing.
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