Probing the Inhibition of Microtubule Affinity Regulating Kinase 4 by N-Substituted Acridones.

ABSTRACT: Microtubule affinity regulating kinase 4 (MARK4) becomes a unique anti-cancer drug target as its overexpression is responsible for different types of cancers. In quest of novel, effective MARK4 inhibitors, some acridone derivatives were synthesized, characterized and evaluated for inhibitory activity against human MARK4. Among all the synthesized compounds, three (7b, 7d and 7f) were found to have better binding affinity and enzyme inhibition activity in µM range as shown by fluorescence binding, ITC and kinase assays. Here we used functional assays of selected potential lead molecules with commercially available panel of 26 kinases of same family. A distinctive kinase selectivity profile was observed for each compound. The selective compounds were identified with submicromolar cellular ac

SUBMITTER: Voura M 

PROVIDER: S-EPMC6368574 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature