There are more than 500 protein kinase inhibitors in our bodies that are responsible for cellular maintenance and cellular growth.

However, some of that cellular growth can be harmful when it comes to cancer cells. Genetically mutated kinases accelerate cancer cells and can even be the cause for a number of life threatening cancers such as Abelson murine leukemia.

San Diego State University chemist, Jeffrey Gustafson, has identified a new way for improving the selectivity of protein kinase inhibitors and possibly decreasing unwanted side effects by developing new science to slow down the overactive kinases. His research was recently published in a top chemistry journal Angewandte Chemie.

“It’s extremely difficult to inhibit or weed out the off-target kinases because kinases are “cookie cutter” proteins that can inhibit 20-30 other kinases causing unwanted side effects,” Gustafson said in the journal.

In the study, Gustafson and his team were able to increase selectivity and reduce unwanted side effects such as nausea, headaches and heart attacks for patients that are undergoing the therapeutic use. This was a watershed moment for the team because it meant a future in treating cancers by targeting specific kinases.

“We want to give inhibitors the address of what kinases to inhibit to lower the count of side effects and be more selective,” Gustafson said.

This is new science that can have a breakthrough in cancer research.

Many kinase inhibitors have axes of chirality that are in rotation around a carbon carbon bond. The scientists created a way to put the brakes on the freely spinning molecule to stop the rotation in a right-handed or a left-handed version. Both of these forms behave differently. It’s a roulette where one form can target 16 percent of kinases and the other form can target 10 percent, which is significantly lower than the average of 44 percent with higher increases of side effects for patients.

This will be an ongoing project for Gustafson who wishes to work toward getting an FDA approved drug on the market. Currently, there are 25 FDA approved drugs that use some form of kinase inhibitors, but his team was the first to make a distinction between kinases to increase selectivity of kinase inhibitors that can lead to a reduction of side effects.

Research, such as this by Gustafson, increases oncology efforts toward the creation of new drugs, reducing side effects and extending the lives of cancer patients. In conjunction with SDSU’s long-term strategic plan, “Building on Excellence,” this study enhances the university as an R1 university in the same research designation as other top-tier research universities. Studies such as these can help the university rise up in rank and be part of the top 50 public research universities in the nation.