Cobalt amine complexes and Ru265 interact with the DIME region of the mitochondrial calcium uniporter

We report our investigation into the MCU-inhibitory activity of Co 3+ complexes in comparison to Ru265. These compounds reversibly inhibit the MCU with nanomolar potency. Mutagenesis studies and molecular docking simulations suggest that the complexes operate through interactions with the DIME motif...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2021-06, Vol.57 (5), p.6161-6164
Hauptverfasser: Woods, Joshua J, Rodriguez, Madison X, Tsai, Chen-Wei, Tsai, Ming-Feng, Wilson, Justin J
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Sprache:eng
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Zusammenfassung:We report our investigation into the MCU-inhibitory activity of Co 3+ complexes in comparison to Ru265. These compounds reversibly inhibit the MCU with nanomolar potency. Mutagenesis studies and molecular docking simulations suggest that the complexes operate through interactions with the DIME motif of the MCU pore. The MCU-inhibitory properties and mechanisms of action of Co 3+ amine complexes and Ru265 are described.
ISSN:1359-7345
1364-548X
DOI:10.1039/d1cc01623g