Preclinical studies of celastrol and acetyl isogambogic acid in melanoma.

ABSTRACT:

Purpose

Sensitize melanomas to apoptosis and inhibit their growth and metastatic potential by compounds that mimic the activities of activating transcription factor 2 (ATF2)-driven peptides.

Experimental design

Small-molecule chemical library consisting of 3,280 compounds was screened to identify compounds that elicit properties identified for ATF2 peptide, including (a) sensitization of melanoma cells to apoptosis, (b) inhibition of ATF2 transcriptional activity, (c) activation of c-Jun NH(2)-terminal kinase (JNK) and c-Jun transcriptional activity, and (d) inhibition of melanoma growth and metastasis in mouse models.

Results

Two compounds, celastrol (CSL) and acetyl isogambogic acid, could, within a low micromolar range, efficiently elicit cell death in melanoma cel

SUBMITTER: Abbas S 

PROVIDER: S-EPMC2874065 | biostudies-literature | 2007 Nov

REPOSITORIES: biostudies-literature