RRC ID 61680
著者 Tsuganezawa K, Sekimata K, Nakagawa Y, Utata R, Nakamura K, Ogawa N, Koyama H, Shirouzu M, Fukami T, Kita K, Tanaka A.
タイトル Identification of small molecule inhibitors of human COQ7.
ジャーナル Bioorg Med Chem
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.
巻・号 28(1)
ページ 115182
公開日 2020-1-1
DOI 10.1016/j.bmc.2019.115182
PII S0968-0896(19)31618-9
PMID 31753803
MeSH Antineoplastic Agents / chemical synthesis Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Cell Proliferation / drug effects Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Enzyme Inhibitors / chemical synthesis Enzyme Inhibitors / chemistry Enzyme Inhibitors / pharmacology* HeLa Cells Humans Mitochondrial Proteins / antagonists & inhibitors* Mitochondrial Proteins / metabolism Mixed Function Oxygenases / antagonists & inhibitors* Mixed Function Oxygenases / metabolism Molecular Structure Small Molecule Libraries / chemical synthesis Small Molecule Libraries / chemistry Small Molecule Libraries / pharmacology* Structure-Activity Relationship Tumor Cells, Cultured
IF 3.073
リソース情報
ヒト・動物細胞 WI-38(RCB0702) HeLa