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Scripps Research and MIT scientists discover class of potent anti-cancer compounds
Date:3/7/2011

velop a PME-1 inhibitor, mainly because standard substrate assays for the enzyme were difficult to adapt for high-throughput screening," said Cravatt. "But we believed that we could use our new 'substrate-free' screening technology for PME-1; and we knew that we needed to try a large, high-throughput screen, because our small-scale efforts to find PME-1 inhibitors had come up empty."

Scripps Research runs an NIH Molecular Libraries Program screening center at its Jupiter, Florida campus. There, the institute's researchers set up an automated version of Bachovchin's new screening technique and used it to search for strong PME-1 inhibitors among the 300,000-plus small-molecule compounds in the NIH library.

Super Potent, Super Selective

Like many molecules, ABLs can exist in two mirror-image versions, known as enantiomers, and they usually are synthesized as an equal mixture of both compounds. But Fu and his group had used new chemistry techniques to produce the ABLs in an "enantiomerically selective" way, in case one enantiomer of a compound had more activity than its mirror-image twin. And, in fact, one of these enantiomeric molecules, ABL127, turned out to fit so precisely into a nook on PME-1 that it completely blocked PME-1 activity in cell cultures and in the brains of mice. Aside from being extremely potent, it also was highly selective for PME-1, so that even at higher doses, it had negligible effects on other enzymes in the PME-1 family, known as serine hydrolases. In mice, ABL127's inhibition of PME-1 activity caused a more than one-third drop in the measured level of demethylated ("inactive") PP2A.

The Cravatt and Fu labs are now working together to synthesize more ABLs and explore their chemistry, looking for the best possible PME-1 inhibitor. The near-term goal is to use ABL127 as a scientific probe to study PME-1 functions in animals. A longer-term goal is to develop ABL127, or related compounds, as potential oncolo
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Contact: Mika Ono
mikaono@scripps.edu
858-784-2052
Scripps Research Institute
Source:Eurekalert

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