Identification of small molecule inhibitors of human COQ7.

Keiko Tsuganezawa, Katsuhiko Sekimata, Yukari Nakagawa, Rei Utata, Kana Nakamura, Naoko Ogawa, Hiroo Koyama, Mikako Shirouzu, Takehiro Fukami, Kiyoshi Kita, Akiko Tanaka

Bioorganic & medicinal chemistry 2020 Jan 01

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Given that the associated clinical manifestations of ubiquinone (UQ, or coenzyme Q) deficiency diseases are highly heterogeneous and complicated, effective new research tools for UQ homeostasis studies are awaited. We set out to develop human COQ7 inhibitors that interfere with UQ synthesis. Systematic structure-activity relationship development starting from a screening hit compound led to the identification of highly potent COQ7 inhibitors that did not disturb physiological cell growth of human normal culture cells. These new COQ7 inhibitors may serve as useful tools for studying the balance between UQ supplementation pathways: de novo UQ synthesis and extracellular UQ uptake. Copyright © 2019 Elsevier Ltd. All rights reserved.

Citation

Keiko Tsuganezawa, Katsuhiko Sekimata, Yukari Nakagawa, Rei Utata, Kana Nakamura, Naoko Ogawa, Hiroo Koyama, Mikako Shirouzu, Takehiro Fukami, Kiyoshi Kita, Akiko Tanaka. Identification of small molecule inhibitors of human COQ7. Bioorganic & medicinal chemistry. 2020 Jan 01;28(1):115182