Selective Inhibitors For Cyclin-Dependent Kinases

Emory University
posted on 07/07/2009

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Applications

Development of novel, highly selective cyclin-dependent kinase (CDK) inhibitors for the treatment of diseases.

Highlights

• Efficient, high-yielding synthesis of pyrazolo[1,5-a]pyrimidine derivatives.
• Potential as breast cancer treatments due to highly selective CDK7 inhibition.
• Ability to treat a variety of diseases resulting from inappropriate activity of CDKs.

Technical Summary

Cyclin-dependant kinases (CDKs) are the catalytic subunits of a large family of serine/threonine protein kinases that are integrally involved in a variety of cellular processes. Because of the role of specific CDKs in the regulation of the cell cycle, they have been identified as important targets for the design of drugs with antimitotic, antineurodegenerative, antiviral, and antitumor effects.

Emory researchers, along with colleagues from Imperial College in London, have developed a series of pyrazolo[1,5-a]pyrimidine compounds that are useful for the selective inhibition of cyclin-dependent kinases. The compounds are potential therapeutics for diseases resulting from inappropriate activity of kinases, including cancer, viral infections, neurodegenerative disorders, and cardiovascular disorders. Certain members of the class have demonstrated specific inhibition of CDK7, which makes them especially suitable for the treatment of breast cancer.

Developmental Stage & Potential Market

• In vitro assays have been performed to determine the level of inhibition against various kinases. Lead compounds have been identified.
• The worldwide market for cancer therapeutics stands at more than $20 billion, with annual growth rates of 15%-20%. Inhibitors of CDKs are important drug candidates because of their potential to restore the inhibitory control of the cell cycle that is frequently lost in cancer cells.