Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.
Basic Information
ID: ALA3797047
Journal: Bioorg Med Chem Lett
Title: Discovery of indirubin derivatives as new class of DRAK2 inhibitors from high throughput screening.
Authors: Jung ME, Byun BJ, Kim HM, Lee JY, Park JH, Lee N, Son YH, Choi SU, Yang KM, Kim SJ, Lee K, Kim YC, Choi G.
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 (IC50=0.003μM). We also propose that compound 16 may bind to the ATP-binding site of the enzyme based on enzyme kinetics and molecular docking studies.
CiteXplore: 27106709
DOI: 10.1016/j.bmcl.2016.03.111
Patent ID: ┄