AI-10-49

AI-10-49

AI-10-49 is a small molecule inhibitor that specifically targets the BRD4 protein, a member of the BET (bromodomain and extra-terminal) family of proteins. It was developed by researchers at the Dana-Farber Cancer Institute and is currently being studied for its potential use in the treatment of various types of cancer.

Mechanism of Action

AI-10-49 works by binding to the bromodomains of BRD4, thereby inhibiting the protein's ability to bind to acetylated histones. This disrupts the normal function of BRD4, which plays a key role in the regulation of gene expression by modulating the structure of chromatin. By inhibiting BRD4, AI-10-49 can potentially alter the expression of genes that are involved in the growth and proliferation of cancer cells.

Potential Therapeutic Applications

The therapeutic potential of AI-10-49 is currently being explored in preclinical studies. Early research suggests that it may be effective in treating various types of cancer, including leukemia, lymphoma, and solid tumors. In particular, it has shown promise in treating cancers that are driven by the overexpression or mutation of the MYC oncogene, which is a common feature of many aggressive cancers.

Clinical Development

As of now, AI-10-49 is still in the early stages of clinical development. Further studies are needed to determine its safety, efficacy, and optimal dosing regimen in humans. However, the initial results from preclinical studies are promising and suggest that it may have significant potential as a novel cancer therapy.

See Also

• BET inhibitor
• Epigenetics in cancer
• Targeted therapy