AI Article Synopsis
- * Blocking the TGF-β signaling pathway could be an effective way to treat cancer.
- * A new series of thiazole compounds was discovered, with one—compound 29b—showing strong inhibition of the ALK5 kinase, which is crucial for TGF-β signaling, at a low concentration of 3.7 nM and with good selectivity for the kinase.
Article Abstract
TGF-β is an immunosuppressive cytokine and plays a key role in progression of cancer by inducing immunosuppression in tumor microenvironment. Therefore, inhibition of TGF-β signaling pathway may provide a potential therapeutic intervention in treating cancers. Herein, we report the discovery of a series of novel thiazole derivatives as potent inhibitors of ALK5, a serine-threonine kinase which is responsible for TGF-β signal transduction. Compound 29b was identified as a potent inhibitor of ALK5 with an IC value of 3.7 nM with an excellent kinase selectivity.
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| http://dx.doi.org/10.1016/j.bmcl.2024.129797 | DOI Listing |
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