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Pinning protein could answer provocative cancer question
Date:10/30/2012

HOUSTON -- (Oct. 29, 2012) -- Answers are often elusive in the fight against cancer, and Rice University chemist Zachary Ball is hoping to pin one down -- with pins made of single atoms. The work, which aims to create a drug that's effective against an "undruggable" protein, is one of the first 50 proposals funded under the National Cancer Institute's (NCI) Provocative Questions Project.

The Provocative Questions Project, in its inaugural year, is designed to spur innovative approaches to critical questions that could, if answered, substantially change the way scientists approach cancer research. Ball, assistant professor of chemistry at Rice, and collaborators at Baylor College of Medicine (BCM) are attempting to answer one of 24 questions posed by NCI: "Are there new technologies to inhibit traditionally 'undruggable' target molecules, such as transcription factors, that are required for (cancer)?"

"Most drugs are small molecules that bind tightly to a protein and literally get in the way of it sticking to whatever it might normally interact with, often another protein," Ball said. "Drugs tend to be small molecules because those are the easiest to introduce into cells and because small molecules are particularly effective at binding tightly into the tiny pockets that exist on many proteins."

Unfortunately, there are some proteins that don't have the tiny pockets favored by drug designers. By some estimates, small-molecule drugs are ineffective against as many as 80 percent of the proteins in human cells, including many signaling proteins and a class of proteins called transcription factors that help control basic functions like cell death and cell reproduction. Drugmakers often call these proteins "undruggable."

"Researchers have actually spent a good deal of time and effort looking for drug candidates that are effective against some of these undruggable targets," Ball said. "But the results are generally mediocre, and af
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Contact: Jade Boyd
jadeboyd@rice.edu
713-348-6778
Rice University
Source:Eurekalert  

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