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Fox Chase researchers discover a method for clamping down on a cancer-promoting enzyme
Date:4/18/2008

d his Fox Chase colleagues looked for new molecules that inactivate PAK1 in other ways. The cancer drug Gleevec, for example, is unusually selective for its target by binding to a region outside of the active site that is less common among kinases.

Many other kinases, including PAK1, have unique regions outside the active site that mediate important facets of their function such as localization, substrate recruitment, or regulation, Peterson says. We wondered whether these regions might offer other places for molecules to bind and inhibit PAK1 without affecting other enzymes.

According to Peterson, IPA-3 achieves high selectivity for PAK1 by taking advantage of a unique self-regulating region of the enzyme. The PAK1 protein has an auto-regulatory arm, a structure that PAK1 folds over its own active site when the enzyme is not in use. Their findings suggest that IPA-3 binds to the protein when it is in the closed configuration, which then prevents PAK1 from becoming active.

It is like when the Steve Irwin would subdue a crocodile, he would tape its jaws closed to keep it from biting, Peterson says. Likewise, IPA-3 latches onto PAK1 in a way that prevents PAK1 from exposing its active site.

Peterson and his colleagues, found IPA-3 by screening a library of over 33,000 small molecules for their ability to block phosphorylation by pure PAK1 protein. Any small molecules that blocked PAK1 were noted and were then ranked by potency, reproducibility and commercial availability. IPA-3 came out ahead of the others through this winnowing process, and the researchers then tested IPA-3 to demonstrate that it could also inhibit PAK1 activity inside living cells.

The Fox Chase researchers believe that IPA-3 represents a promising new strategy for creating therapeutics that inhibit PAK1 by mimicking the way cellular enzymes self-regulate in real life, but the IPA-3 molecule itself is not suitable as a therapeutic in its current f
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Contact: Greg Lester
gregory.lester@fccc.edu
215-728-2753
Fox Chase Cancer Center
Source:Eurekalert

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