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Gene & Protein in Disease TOPK: Target for lung cancer treatment

Treatment Targeted treatment 30 Combined with 5-FU 19 Targeted treatment 30 Combined with radiotherapy 56 Targeted treatment 38 Targeted treatment 40 Targeted treatment 47 Targeted treatment 46

Efficacy TGIs of 90.3% (2.5 mg/kg) and 99.8% (5 mg/kg) Inducing apoptosis synergistically TGIs of 110% (40 mg/kg) Enhancing tumor sensitivity to fractionated irradiation N/A Growing remarkably; more slowly with 50-mg/kg baicalin Significant inhibition Suppressing tumor growth

1,2.5 and 5 mg/kg 5-FU (100 mg/kg) 40 mg/kg OTS964 (20 mg/kg) Gulmay (2 Gy/min) N/A 20 or 50 mg/kg 20 mg/kg 25 mg/kg
Dose OTS514 (2.5 mg/kg)

Human lung cancer Human lung cancer Human lung cancer Human lung cancer Human lung cancer Human lung cancer Human lung cancer

In vivo xenograft model xenograft model xenograft model xenograft models N/A xenograft model xenograft model xenograft model

Table 1. Information of a selection of TOPK inhibitors and their efficacy against lung cancer

Concentration OTS514 (20 nM) ICM scores = −31.88 Kd = 111.0 ± 2.3 μM IC 50 =30.10 – 148.21 μM 10, 20, and 50 μM IC 50 =4.823 μM 0, 5, 10, 15, 20 μM

N/A 5-FU (25 μM) IC 50 =31 nM IC 50 =7.6 nM 10 or 20 nM 5,7.5,10 µM

A549 and LU-99 cell lines A549 cell lines A549 cell lines LU-99 cell lines H460 cell lines Calu-6 cell lines Virtual ligand screening A549 cell lines Kinase assay Kinase assay A549 cell lines Kinase assay Abbreviations: 5-FU: Fluorouracil; TGI: Tumor growth inhibition; TOPK: T-LAK cell-originated protein kinase.
In vitro

Chemical structure

Name OTS514 OTS964 Ilaprazole Baicalin Glycerol Xanthohumol

Volume 3 Issue 2 (2024) 6 doi: 10.36922/gpd.3062