Journal
FUTURE MEDICINAL CHEMISTRY
Volume 11, Issue 13, Pages 1523-1536Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0448
Keywords
dimethyl fumarate; docking studies; fibrosis; heme oxygenase-1; Keap1; lung; NMR; Nrf2
Categories
Ask authors/readers for more resources
Aim: Dimethyl fumarate (DMF) analogs were synthesized to obtain inducers of HO-1 and antifibrotic agents. Methods: HO-1 expression levels were measured on lung fibroblasts (MRC5). NMR and docking studies were performed. Heme oxygenase activity, gene levels and protein expression have been measured for the most active compound 1a. Collagen production by fibroblast after exposure to TGF-ss was measured. Results: Compound 1a showed to be a strong HO-1 inducer. Its activity seems to be mediated by activation of nuclear factor erythroid 2 related factor 2 (Nrf2). TGF-ss-induced collagen production was significantly decreased on MRC5, pretreated with DMF or 1a. DMF and 1a have a high potential for treatment of lung fibrotic injuries. [GRAPHICS] .
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available