| Autor: |
Henry I C, Lowe, Caroline O B, Facey, Ngeh J, Toyang, Joseph L, Bryant |
| Rok vydání: |
2014 |
| Předmět: |
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| Zdroj: |
Anticancer research. 34(4) |
| ISSN: |
1791-7530 |
| Popis: |
The Jamaican "Guinea Hen Weed" (Petiveria alliacea L.) plant has been traditionally used in folklore medicine to treat a variety of diseases including cancer. In the present study we investigated on the therapeutic feasibility of dibenzyl trisulfide (DTS) (isolated from the Jamaican Guinea Hen Weed) as a potent small-molecule kinase inhibitor to treat cancer.We investigated the inhibitory effects of DTS against a large panel of kinases using a well-established competitive binding assay. Cell proliferation data were obtained using the WST-1 colorimetric assay.DTS inhibited the activity of the C-terminal kinase domain of RSK1 (80% compared to control) with a Kd of 1.3 μM. Anti-proliferative effects of DTS were observed in small lung, pancreatic, breast, and prostate cancer cells with IC50 values ranging from 0.34-0.84 μM.We have identified DTS as a highly selective and isoform-specific RSK1 kinase inhibitor with broad cancer therapeutic potential. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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