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Identification of small molecule inhibitors of human COQ7.
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2019-11-09 , 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 1
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2019-11-09 , 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 1
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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.
中文翻译：
鉴定人COQ7的小分子抑制剂。
鉴于泛醌（UQ或辅酶Q）缺乏症的相关临床表现高度异质且复杂，因此需要有效的新研究工具进行UQ稳态研究。我们着手开发可干扰UQ合成的人COQ7抑制剂。从筛选命中化合物开始的系统结构与活性关系的发展导致鉴定了高效的COQ7抑制剂，该抑制剂不会干扰人类正常培养细胞的生理细胞生长。这些新的COQ7抑制剂可作为研究UQ补充途径（从头UQ合成和细胞外UQ摄取）之间平衡的有用工具。
更新日期：2019-11-11
中文翻译：
鉴定人COQ7的小分子抑制剂。
鉴于泛醌（UQ或辅酶Q）缺乏症的相关临床表现高度异质且复杂，因此需要有效的新研究工具进行UQ稳态研究。我们着手开发可干扰UQ合成的人COQ7抑制剂。从筛选命中化合物开始的系统结构与活性关系的发展导致鉴定了高效的COQ7抑制剂，该抑制剂不会干扰人类正常培养细胞的生理细胞生长。这些新的COQ7抑制剂可作为研究UQ补充途径（从头UQ合成和细胞外UQ摄取）之间平衡的有用工具。
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