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Company, Institute Partner on Cancer Drug Candidate Catalog

Chemotherapy (National Institutes of Health)

(National Institutes of Health)

Researchers at Fox Chase Cancer Center in Philadelphia and Reaction Biology Corporation in Malvern, Pennsylvania have compiled an index of 178 candidate drugs capable of blocking the activity of one or more of 300 enzymes, including enzymes involved with cancer. Their findings appear online in the journal Nature Biotechnology, and are also scheduled for publication in the journal’s November 2011 print issue (paid subscription required).

The enzymes, called kinases, act as catalysts for a number of biological activities, which include drivers for many forms of cancer. The candidate drugs, called kinase inhibitors, thus have the potential to act as anti-cancer agents. Because of their effects on multiple biological functions, however, they can also interfere with normal processes in the body, resulting in side effects.

These compounds, including inhibitors of all major kinase families, were then profiled against 300 human kinases, also representing all major kinase families. An analysis of the results showed that many kinase inhibitors had significant and up-to-now unknown off-target effects, inhibiting enzymes belonging to the same subfamilies as their intended targets, but also inhibiting kinases from completely different families.

Six compounds, in particular, had off-target inhibition effects stronger than the intended target, which supports the importance of profiling compounds against a range of kinases before starting animal studies or clinical trials. With the new library, researchers will be able to analyze complex interactions of these inhibitors with their targets to develop cancer drugs that block specific kinases responsible for disease, while seeking to avoid major side effects.

Reaction Biology and Fox Chase have made the catalog of compounds and kinases available to the research community on the Web. Haiching Ma, Reaction Biology’s chief technology officer, notes that the catalog will have value beyond the immediate needs of drug researchers. “This data set will not only help drug discovery activity in the industry,” says Ma, “but also provide guidance for selecting the right tool compounds for use in routine kinase biology studies.”

Read more: Online Cancer Genomics Tool for Clinicians Unveiled

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