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Fig. 1. Screening of JNK-JIP1 interaction inhibitors. (A) Illustration of FRET fluorescence analysis with JNK-CFP and JIP1-YFP. (B) FRET assay was performed as indicated in methods. 0.001% Dimethyl sulfoxide (DMSO) is a vehicle control and Cyproterone acetate (CPA) was used as negative control. BI-78D3 (BI), a known inhibitory compound of JNK-JIP1 complex, was used as positive control. Compound candidates were named by abbreviations, Acebutolol (AC), Lithium chloride (LICL), Vincristine sulfate (VCR), Niacinamide (NAA), Valproic acid (VPA), Dihydro ouabain (DHO), Ethylisopropylamiloride (EIPA), Chloroquine diphosphate (CDP), Homosalate (HMS), Enilconazole (ENIL), Sertraline (SRT), 5-aminovaleric acid (5AVA), Methocarbamol (MCBL), Quinapril (QUI), Oseltamivir (OTV), Nitrofurantoin (NTF), Homatropine bromide (HB), Propranolol (PRO), JLK6, Indirubin-3′-monoxime (I3MO), Hydroquinone (HQ), O(6)-benzylguanine (O6BG), N-bromoacetamide (NBA), PK 11195, Nifedipine (NIF), Probenecid (PROB), Yohimbine hydrochloride (YOH), Zacoprode (ZAC), Ranitidine hydrochloride (RANH). The bar graph shows relative FRET intensity of the mean ratio of the FRET versus CFP from three independent experiments. Statistical analysis was assessed by one-tailed unpaired t-test; n=3; *p<0.05, **p<0.01, ***p<0.001 vs. DMSO. (C) JNK-CFP (upper panel) and JIP1-YFP plasmids were co-transfected in 293A cells, and then candidate compounds (1 μM) were treated for 1 h. DMSO represents the vehicle control with 0.001% DMSO. Cyproterone acetate (CPA) is one of the non-effective compounds used as a negative control and BI-78D3 (BI) used as the positive control. FRET fluorescence (lower panel) shows intensity of JNK-JIP1 interaction.
Biomolecules & Therapeutics 2018;26:458~463 https://doi.org/10.4062/biomolther.2017.123
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