Abstract
Cucurbitacins (Cucs) have been classified as signal transducer and activator of transcription 3 inhibitors. Kinase inhibition has been a validated drug target in multiple types of malignancies. B-RAF mutations are highly expressed in the melanoma. Our hypothesis is the Cucs can be a potential candidate to inhibit the signaling kinase pathway. The research presented is the evaluation of Cucs, as B-RAF and MEK1 kinase inhibitors. Virtual screening methods were employed to identify lead compounds. The hypothesis was tested on mutant B-RAF cell lines, A-375 and Sk-Mel-28 cell lines to determine the activity toward melanoma. A series of natural Cucs show an improved activity toward Sk-Mel-28 and A-375 cell lines. Cucs show potential inhibition for the total and phosphorylated ERK using ELISA kits. Cucs could be potential candidate for inhibiting cell growth.
Original language | English (US) |
---|---|
Pages (from-to) | 162-167 |
Number of pages | 6 |
Journal | Journal of Enzyme Inhibition and Medicinal Chemistry |
Volume | 29 |
Issue number | 2 |
DOIs | |
State | Published - Apr 2014 |
Externally published | Yes |
Keywords
- Cucurbitaceae
- MEK
- Mutant B-RAF
- Triterpenoids
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery