Fig. 3.
Desloratadine exerts anticancer bioactivity by directly binding to Asn-246 of the NMT1 protein. a SDS-PAGE and Western blot analysis indicating the purification of the NMT1 protein. b SPR analysis showing the affinity of desloratadine for the NMT1 protein. c SK-Hep1-shCON, SK-Hep1-shNMT1, Hep3B-shCON, and Hep3B-shNMT1 cells were treated with 6 µg/ml desloratadine or DMSO, and cell viability was evaluated using a CCK-8 assay. d A total of 5 × 106 HCC cells (Hep3B-shCON or Hep3B-shNMT1) were inoculated into nude mice (n = mice 6 per group). Tumor-bearing mice were treated with desloratadine (15 mg/kg) or an equal volume of vehicle. e Representative images of Ki67 staining in tumor tissue. f The binding of NMT1 with desloratadine was investigated by molecular docking simulation. g Detection of NMT1 protein expression in each generated cell line by Western blot. h Cells expressing mutant or wild-type NMT1 were treated with 6 µg/ml desloratadine or DMSO, and cell viability was evaluated using a CCK-8 assay. i Expression and purification of the NMT1N246A mutant protein in a prokaryotic expression system. j Detection of the binding of NMT1N246A to desloratadine by SPR analysis, with wild-type NMT1 as the control. Bars, SDs; *p < 0.05; **p < 0.01, ***p < 0.001