Cucurbitacins: Potential candidates targeting mitogen-activated protein kinase pathway for treatment of melanoma

Mahmoud S. Ahmed, Fathi T. Halaweish

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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 languageEnglish (US)
Pages (from-to)162-167
Number of pages6
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume29
Issue number2
DOIs
StatePublished - Apr 2014
Externally publishedYes

Keywords

  • Cucurbitaceae
  • MEK
  • Mutant B-RAF
  • Triterpenoids

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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