Fig. 1: Screening for small-molecule compounds that inhibit Mint3.
From: Pharmacological inhibition of Mint3 attenuates tumour growth, metastasis, and endotoxic shock
a Schematic illustration of the screening process for Mint3 inhibitors. Mint3-binding compounds were identified using chemical arrays in the first screening. Then, using the luciferase assay in the second screening, hit compounds were tested to determine whether they inhibited HIF-1 transcriptional activity. b Structure of the hit compound, NPD7801 (compound #1). c Luciferase assay of HIF-1 activity in HT1080 cells treated with compound #1 at the indicated concentrations. d Luciferase assay of HIF-1 activity in HT1080 cells treated with 10 μM compound #1 and the analogues of compound #1 (#2–19). $ indicates no detection of luciferase activity due to cell death. e Structure of NPD8369 (compound #19), naphthofluorescein (Naph). f Luciferase assay for HIF-1 activity in HT1080 cells treated with DMSO or Naph at the indicated concentrations for 24 h. In (c), (d), and (f), error bars indicate SD (n = 3). Data were analysed using Student’s t test. *p < 0.05, **p < 0.01, ***p < 0.001.
