JQ1

JQ1

JQ1 is a small molecule inhibitor that targets the Bromodomain and Extra-Terminal motif (BET) family of proteins, specifically BRD4. It was first developed by the research group of James E. Bradner at the Dana-Farber Cancer Institute and has been widely used in preclinical research to study the role of BET proteins in various diseases, including cancer, inflammation, and cardiovascular disease.

Structure and Mechanism of Action

JQ1 is a thieno-triazolo-1,4-diazepine that binds to the bromodomains of BET proteins, preventing them from interacting with acetylated histones. This disrupts the ability of BET proteins to regulate gene expression, leading to changes in cellular behavior.

Applications in Research

JQ1 has been used in a wide range of preclinical studies to investigate the role of BET proteins in disease. For example, it has been shown to inhibit the growth of various types of cancer cells, including those from leukemia, melanoma, and lung cancer. It has also been used to study the role of BET proteins in inflammation and cardiovascular disease.

Clinical Development

While JQ1 itself is not currently in clinical development, it has served as a prototype for the development of other BET inhibitors that are being tested in clinical trials for various types of cancer and other diseases.

Safety and Side Effects

As a research tool, JQ1 is not intended for use in humans and its safety profile has not been fully evaluated. However, studies in animals have suggested that it may have potential side effects, including weight loss and decreased fertility.

See Also

• Bromodomain
• Epigenetics
• Histone deacetylase inhibitor

This article is a stub related to pharmacology. You can help WikiMD by expanding it!

   This article is a oncology stub. You can help WikiMD by expanding it!