A unique library representing an important new tool for accelerating the development of an entire class of targeted cancer drugs has been created by scientists at Fox Chase Cancer Center. The actions of 178 candidate drugs capable of blocking the activity of one or more of 300 enzymes, including enzymes critical for cancer, have been cataloged and cross-indexed. The new library allows researchers the ability to analyze the complex interactions of these kinase inhibitors with their targets and thus develop cancer drugs that block specific kinases responsible for disease, while working to avoid major drug side effects.
“These results have pushed the field closer to finding truly specific inhibitors of the processes that drive cancer,” says Jeffrey R. Peterson, PhD, associate professor in the Cancer Biology Program at Fox Chase and senior author on the new study. “We now have a collection of kinase inhibitors that are more well-characterized and understood than any other library. The next step is to use this information to identify specific, effective therapies that stop cancer in its tracks while avoiding healthy processes.” Researchers published the library of results on a free Web site.
Peterson says cataloging the activity of 178 kinase inhibitors against 300 kinases was like observing what happens after shooting a scattergun at a wall of balloons. Before, scientists could only tell if one particular balloon popped. Now, it’s possible to determine if other balloons were hit as well. “We’re essentially shining a light on the wall of balloons so we have a much better view of the balloons that were popped,” said Peterson.
Initially, the goal was to find an inhibitor that targets one specific kinase involved in cancer. Instead, scientists discovered that multiple kinases likely work together to produce the disease. So stopping the cancer process involves hitting all of those kinases together.
By using the data, inhibitors that act on particular cancer-promoting kinases have already been identified. Therefore, researchers may soon be able to modify current therapies so the drug treatments target only those specific kinases involved in cancer, while avoiding kinases unrelated to the disease.
Source: Fox Chase Cancer Center.