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Enzyme structure reveals new drug targets for cancer and other diseases
Date:2/14/2008

havior of p300/CBP will help scientists design a p300/CBP inhibitor that might function in human cells as an anticancer drug.

Proper functioning of p300/CBP is critical for insulin regulation and the health of heart cells. As a result, compounds that can regulate p300/CBP activity might be useful in the treatment of diabetes and heart disease.

In addition, HAT activity is necessary for the multiplication of HIV, leading at least one scientific group to suggest that targeting HATs or similar enzymes might be an new way to thwart the virus.

Finally, the article also shows that some p300/CBP mutations previously linked to certain cancers lie right where p300/CBP contacts the inhibitor. Studying how these mutations alter the enzyme's function should shed light on why the mutations can lead to disease.

"This work illustrates how enzymology and structural biology can combine to yield both fundamental and practical insights about an important biomedical problem. The studies provide a new framework for understanding p300/CBP in health and disease," said Jeremy M. Berg, NIGMS Director.


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Contact: Alisa Machalek
alisa.machalek@nih.gov
301-496-7301
NIH/National Institute of General Medical Sciences
Source:Eurekalert

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