期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 7, 页码 2200-2209出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.02.035
关键词
RNA helicase; Eukaryotic initiation factor 4A3 (eIF4A3) inhibitors; Exon junction complex (EJC); ATP-competitive type inhibitors; Isothermal titration calorimetry (ITC); Surface plasmon resonance (SPR)
Eukaryotic initiation factor 4A3 (eIF4A3), an ATP-dependent RNA helicase, is a core component of exon junction complex (EJC). EJC has a variety of roles in RNA metabolism such as translation, surveillance, and localization of spliced RNA. It is worthwhile to identify selective eIF4A3 inhibitors with a view to investigating the functions of eIF4A3 and EJC further to clarify the roles of the ATPase and helicase activities in cells. Our chemical optimization of hit compound 2 culminated in the discovery of ATP-competitive eIF4A3 inhibitor 18 with submicromolar ATPase inhibitory activity and excellent selectivity over other helicases. Hence, compound 18 could be a valuable chemical probe to elucidate the detailed functions of eIF4A3 and EJC. (C) 2017 Elsevier Ltd. All rights reserved.
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