2. Academic Validation
  3. Identification of small molecule inhibitors of human COQ7

Identification of small molecule inhibitors of human COQ7

  • Bioorg Med Chem. 2020 Jan 1;28(1):115182. doi: 10.1016/j.bmc.2019.115182.
Keiko Tsuganezawa 1,  Katsuhiko Sekimata 2,  Yukari Nakagawa 1,  Rei Utata 3,  Kana Nakamura 1,  Naoko Ogawa 1,  Hiroo Koyama 2,  Mikako Shirouzu 1,  Takehiro Fukami 4,  Kiyoshi Kita 5,  Akiko Tanaka 6
Affiliations

Affiliations

  • 1 RIKEN Systems and Structural Biology Center, 1-7-22 Suehiro-cho, Tsurumi, Yokohama 230-0045, Japan; RIKEN Center for Biosystems Dynamics Research, 1-7-22 Suehiro-cho, Tsurumi, Yokohama 230-0045, Japan.
  • 2 RIKEN Center for Sustainable Resource Science, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
  • 3 RIKEN Systems and Structural Biology Center, 1-7-22 Suehiro-cho, Tsurumi, Yokohama 230-0045, Japan.
  • 4 RIKEN Program for Drug Discovery and Medical Technology Platforms, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.
  • 5 School of Tropical Medicine and Global Health, Nagasaki University, 1-12-4, Sakamoto, Nagasaki 852-8523, Japan.
  • 6 RIKEN Systems and Structural Biology Center, 1-7-22 Suehiro-cho, Tsurumi, Yokohama 230-0045, Japan; RIKEN Center for Biosystems Dynamics Research, 1-7-22 Suehiro-cho, Tsurumi, Yokohama 230-0045, Japan. Electronic address: aktanaka@riken.jp.
PMID: 31753803 DOI: 10.1016/j.bmc.2019.115182
Abstract

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.

Keywords

COQ7; CoQ; Inhibitor; UQ; UQ synthesis; Ubiquinone.

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