Dabrafenib, as a Novel Insight into Drug Repositioning Against Secretory Group IIa Phospholipase A2
- Authors
- Jung, Byeongjin; Kim, Jaehong; Bae, Jong-Sup
- Issue Date
- 2016
- Publisher
- ASIAN NETWORK SCIENTIFIC INFORMATION-ANSINET
- Keywords
- Dabrafenib; HUVECs; sPLA2-IIa; inflammation; mice; drug repositioning
- Citation
- International Journal of Pharmacology, v.12, no.4, pp.415 - 421
- Journal Title
- International Journal of Pharmacology
- Volume
- 12
- Number
- 4
- Start Page
- 415
- End Page
- 421
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/9745
- DOI
- 10.3923/ijp.2016.415.421
- ISSN
- 1811-7775
- Abstract
- The screening of bioactive compound libraries can be an effective approach for repositioning FDA-approved drugs or discovering new treatments for human diseases. The expression of secretory group IIa phospholipase A2 (sPLA2-IIa) is enhanced by development of inflammatory disorders. In this study, sPLA2-IIa expression was induced in the lipopolysaccharide (LPS)-stimulated Human Umbilical Vein Endothelial Cells (HUVECs) and mice to evaluate the effect of dabrafenib. This study illustrates drug repositioning with dabrafenib (DAB) for the modulation of sPLA2-IIa expression and activity. Dabrafenib is a B-Raf inhibitor and initially used for the treatment of metastatic melanoma therapy. Results showed that dabrafenib remarkably suppressed the LPS-mediated protein expression and activity of sPLA2-IIa via inhibition of phosphorylation of cytosolic phospholipase A2 (cPLA2) and extracellular signal-regulated kinase (ERK) 1/2. These results demonstrated that dabrafenib might play an important role in the modulation of sPLA2-IIa expression and activity in response to the inflammatory diseases.
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