期刊论文First-in-class casein kinase 1 alpha inhibitors for overcoming treatment related resistance in AML and pancreatic cancer复制

DOI:复制

文献链接:复制

其他信息:

P Janovská, T Radaszkiewicz, M Čulen…
Cancer …, 2025
aacrjournals.org
Abstract Background: Inhibition of Casein kinase 1 alpha (CK1α) represents a new attractive concept for the therapy of acute myeloid leukemia (AML). Despite this, currently available small-molecule CK1α inhibitors lack sufficient activity and selectivity to fully exploit the therapeutic potential of CK1α inhibition. We have developed a series of potent and highly selective CK1 kinase inhibitors, including the most effective CK1α inhibitors to date. They inhibit all CK1α/δ/ε isoforms, blocking both CK1δ, ε-and CK1α-dependent processes, which …