Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) is crucial for normal brain development and its disruption has been linked to various cancers. DYRK1A drives glioblastoma (GBM) progression via stabilization of epidermal growth factor receptor (EGFR). Here we describe two, selective, benzothiazole-derived DYRK inhibitors, FC-2 and FC-3, obtained by structure-activity optimization of a natural product lead. Both compounds inhibit DYRK1A with nanomolar potency…
NOVEL SMALL-MOLECULE INHIBITORS OF THE PROTEIN KINASE DYRK: POTENTIAL THERAPEUTIC CANDIDATES IN CANCER
bioRxiv Cancer Biology | | Venkataramani, P., Elkayam, E., Garg, A., Cheng, K. F., Altiti, A., He, M., Thakur, K., Michalopoulou, E., Gonzalez, C., Van Aelst, L., Pappin, D., Joshua-Tor, L., Al-Abed, Y., Tonks, N. K.
Topics: lung-cancer, skin-cancer, blood-cancer, brain-cancer, research