Vanillin-Isatin Hybrid-Induced MARK4 Inhibition As a Promising Therapeutic Strategy against Hepatocellular Carcinoma.

ABSTRACT: Microtubule affinity-regulating kinase 4 (MARK4) is a serine-threonine kinase that phosphorylates microtubule-associated proteins (MAPs) and increases the microtubule dynamics. Due to its direct involvement in initiation, cell division, progression, and cancer metastasis, MARK4 is considered a potential therapeutic target. Here, we designed, synthesized, and characterized vanillin-isatin hybrids and evaluated their MARK4 inhibitory potential. All of the compounds strongly bind to MARK4 and interact closely with the active site residues. Finally, the compound VI-9 was selected for further investigation due to its high binding affinity and strong MARK4 inhibitory potential. Tau-phosphorylation assay has further confirmed that VI-9 significantly reduced the activity of MARK4. Co

SUBMITTER: Ahmed S 

PROVIDER: S-EPMC11190929 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature