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Anti-hepatocellular carcinoma activity of the cyclin-dependent kinase inhibitor AT7519

Hepatocellular carcinoma (HCC) is one of the most common cancerous tumors and one of the leading causes of death among cancer-related disorders. Chemotherapy is ineffective in HCC patients, and the number of drugs that are in use is limited. Thus, new molecules are needed that could increase the effectiveness of anti-HCC regimens. Here, we show that AT7519, a CDK inhibitor, exerts positive effects on HCC cells: it inhibits proliferation, migration and clonogenicity. Detailed analysis of the transcriptomes of cells treated with this compound indicated that AT7519 affects a substantial portion of genes that are associated with HCC development and progression. Moreover, we showed that the concomitant use of AT7519 with gefitinib or cabozantinib sensitized HCC cells to these drugs. Thus, our research indicates that AT7519 is worth considering in monotherapy for hepatocellular carcinoma patients or in combination with other drugs, e.g., gefitinib or cabozantinib.

 

Comments:

Hepatocellular carcinoma (HCC) is indeed a common and deadly form of cancer, and the limited efficacy of chemotherapy in HCC patients poses a significant challenge. However, your statement highlights a potential breakthrough in the form of AT7519, a CDK inhibitor. The research you mentioned demonstrates several positive effects of AT7519 on HCC cells, including the inhibition of proliferation, migration, and clonogenicity.

Furthermore, the study delved into the transcriptomes of cells treated with AT7519, revealing its impact on a substantial number of genes associated with HCC development and progression. This finding suggests that AT7519 might have a broad effect on the molecular mechanisms involved in HCC.

Another significant aspect of the research is the observation that combining AT7519 with gefitinib or cabozantinib enhances the sensitivity of HCC cells to these drugs. This synergistic effect indicates the potential of using AT7519 in combination therapies to increase the effectiveness of existing treatments for HCC.

Based on these findings, the researchers propose that AT7519 could be a valuable candidate for monotherapy in HCC patients or as part of combination regimens, such as in combination with gefitinib or cabozantinib.

It's important to note that while the results of this research are promising, further studies, including preclinical and clinical trials, would be necessary to validate the efficacy and safety of AT7519 in treating hepatocellular carcinoma.

Related Products

Cat.No. Product Name Information
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also decrease GSK3β phosphorylation. AT7519 induces apoptosis. Phase 2.

Related Targets

GSK-3 Apoptosis related CDK