2. Academic Validation
  3. Glycyrol exerts potent therapeutic effect on lung cancer via directly inactivating T-LAK cell-originated protein kinase

Glycyrol exerts potent therapeutic effect on lung cancer via directly inactivating T-LAK cell-originated protein kinase

  • Pharmacol Res. 2019 Sep;147:104366. doi: 10.1016/j.phrs.2019.104366.
Shangyun Lu 1,  Linhu Ye 1,  Shutao Yin 1,  Chong Zhao 1,  Mingzhu Yan 1,  Xiaoyi Liu 1,  Jinling Cui 1,  Hongbo Hu 2
Affiliations

Affiliations

  • 1 Beijing Advanced Innovation Center for Food Nutrition and Human Health, College of Food Science and Nutritional Engineering, Beijing Key Laboratory for Food Non-thermal Processing, China Agricultural University, Beijing, China.
  • 2 Beijing Advanced Innovation Center for Food Nutrition and Human Health, College of Food Science and Nutritional Engineering, Beijing Key Laboratory for Food Non-thermal Processing, China Agricultural University, Beijing, China. Electronic address: [email protected].
PMID: 31377221 DOI: 10.1016/j.phrs.2019.104366
Abstract

Molecular targeted therapy for non-small cell lung Cancer (NSCLC) has demonstrated promising outcomes. T-lymphokine-activated killer cell-originated protein kinase (TOPK) is found overexpressed in many Cancer types such as NSCLC, and is considered to be an effective target for lung Cancer treatment. In the present study, we found that glycyrol (GC), a representative coumarin compound isolated from licorice, was highly effective against several human NSCLC cell lines in vitro, and significantly suppressed tumor growth in vivo. Mechanistically, we demonstrated that GC can strongly bind to the TOPK protein and inhibited its kinase activity, leading to the activation of apoptotic signaling pathways. The findings of the present study suggest that GC is a novel promising TOPK Inhibitor and this compound deserves to be further investigated for its potential anti-NSCLC activity.

Keywords

Binding affinity; Coumestrol (PubChem CID: 5281707); Demethylsuberosin (PubChem CID: 5316525); Glycycoumarin (PubChem CID: 5317756); Glycyrol; Glycyrol (PubChem CID: 5320083); Kinase inhibitor; Lung cancer; TOPK.

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