Back to Search
Start Over
Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jun2016, Vol. 26 Issue 11, p2719-2723. 5p. - Publication Year :
- 2016
-
Abstract
- DRAK2 is a serine/threonine kinase belonging to the death-associated protein kinase (DAPK) family and has emerged as a promising drug target for the treatment of autoimmune diseases and cancers. To identify small molecule inhibitors for DRAK2, we performed a high throughput screening campaign using in-house chemical library and identified indirubin-3′-monoximes as novel class of DRAK2 inhibitors. Among the compounds tested, compound 16 exhibited the most potent inhibitory activity against DRAK2 (IC 50 = 0.003 μM). We also propose that compound 16 may bind to the ATP-binding site of the enzyme based on enzyme kinetics and molecular docking studies. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 26
- Issue :
- 11
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 114991011
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.03.111