Discovery of furan carboxylate derivatives as novel inhibitors of ATP-citrate lyase via virtual high-throughput screening

[Display omitted] The enzyme ATP citrate lyase (ACL) catalyzes the formation of cytosolic acetyl CoA, the starting material for de novo lipid and cholesterol biosynthesis. The dysfunction and upregulation of ACL in numerous cancers makes it an attractive target for developing anticancer therapies. A...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-02, Vol.27 (4), p.929-935
Hauptverfasser:	Jernigan, Finith E., Hanai, Jun-ichi, Sukhatme, Vikas P., Sun, Lijun
Format:	Artikel
Sprache:	eng
Schlagworte:	ATP Citrate (pro-S)-Lyase - antagonists & inhibitors ATP citrate lyase inhibitor Cancer metabolism Cancer stemness Carboxylic Acids - chemistry Carboxylic Acids - pharmacology Cell Line Drug Discovery Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Furans - chemistry Furoic acid High-Throughput Screening Assays Humans Molecular Docking Simulation Molecular Structure Virtual screening
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