New cancer treatment is gentler
A new option for cancer treatment is just as effective as, but less toxic than similar drugs.
CANCER TREATMENT: Cancer tumours are formed when cells grow uncontrollably. Kinase inhibitors are substances that can inhibit this uncontrolled growth.
Kinase inhibitors are now being used as an alternative to chemotherapy, a treatment that can be very taxing on the body.
Norwegian researchers have now found a new kinase inhibitor that can match the potency of products currently on the market, but with less toxicity than other options.
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Cancer develops when various growth factors attach to specific sites on the cell membrane.
These binding sites on cells are called receptors. Growth factors trigger an enzyme reaction —called a “kinase”— that instructs the cell to divide uncontrollably. Kinase inhibitors stop this signal.
“This may have the potential to be an effective cancer treatment, says Steffen Bugge at NTNU’s Department of Chemistry.
Bugge recently took his doctorate on the development of new kinase inhibitors. He has worked with Associate Professor Bård Helge Hoff and Svein Jacob Kaspersen from the same department, and Associate Professor Eirik Sundby from the Faculty of Technology at Sør-Trøndelag University College.
Their research won “Gullegget” (The Golden Egg) in NTNU’s 2013 idea competition, along with the welcome boost of NOK 1 million. The NTNU Technology Transfer Office judged approximately 50 contest entries in that competition.
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A disadvantage of this treatment is that the body eventually develops immunity to kinase inhibitors, so it is also important to have several different options.
What the researchers did
- Researchers specifically tackled the epidermal growth factor receptor tyrosine kinase (EGFR-TK), and found new inhibitors based on thieno [2,3-d] pyrimidines.
- The researchers were able to create a library of molecules based on effective methods developed in Bugge’s doctoral work. Combining modelling with testing the degree of inhibition of the substances on these receptors, they were able to understand how the substance is bound to the activity site. Then the substances could be rationally optimized for the particular activity.
- More details can be found in the study abstract and Bugge’s slide presentation.
The path to a commercially available drug is long and expensive, but this research has provided greater insight into the impact of different types of kinase inhibitors based on thienopyrimidine. (See fact box.)
The research group is using the knowledge gained from this doctorate to continue developing other classes of EGFR kinase inhibitors.