Series of screening has created a library of possible new drugs that can be used to treat cancer. The activity of 178 enzyme inhibitors has been assessed, catalogued, documented and made available for the scientific community. While it is unsure whether these enzyme inhibitors can be used in cancer treatment, the enormous collection of data is a starting point for new research that could give rise to multiple new drugs for patients that suffer from cancer. The blocked enzymes, called kinases, all have the same basal function, but we were previously unable to systematically assess their function in the body.
A new technique, developed by the Fox Chase Cancer Center, made it possible to measure enzyme activity of kinase inhibitors in more detail than previously possible, resulting in an enormous collection of data. Kinases play a role in many forms of cancer, which makes research in this field very relevant for novel therapies. Now, scientists need to discover which of these drugs inhibits kinases that are overly active in cancer. Preliminary results have already yielded inhibitors for kinases involved with certain types of cancer. Experiments have yet to reveal whether these inhibitors are really useful as anti-cancer drugs, though. Currently, it is known that the 178 kinase inhibitors target a total of 300 kinases in the body.
|Phosphorylation of a protein; ATP is used as energy .|
Kinases function in the cell to relay cellular signals. They work by adding a phosphorus atom to a molecule, which is consequently able to relay the signal further in the cascade, eventually leading to alteration of gene expression. By activating other molecules through phosphorylation, they are often referred to as catalysts. Signaling pathways are prevalent in every cell, to relay information, and kinases are often involved. Because they have a universal function in the body, treating patients with kinase inhibitors often results in side-effects. Not only because a kinase does not only function in letting cancer cells grow, but also plays a role in ordinary, important cellular processes. In addition, many kinase inhibitors target more than one kinase, which highlights that they can have a broad spectrum of actions in the body. Multiple interactions of kinase inhibitors is one of the most important things the scientists from the Fox Chase Cancer Center have found.
|A basic signaling pathway, from outside the cell to inside the cell nucleus.|
While we did not derive any new cancer therapies yet from the dataset, this is a firm step in the right direction. Kinase inhibitors are already used in some forms of cancer, and having 178 new drugs to study will probably reveal a couple of new treatments. Studies to test these newly characterized kinase inhibitors are likely to be underway already.
Currently, cancer is often treated with crude therapies, that do not only kill cancer cells, but also cause harm to healthy cells. Chemotherapy and radiation therapy are examples. Scientists focus on developing molecular strategies, in an attempt to specifically target cancer cells, while leaving healthy cells unharmed. For many years now, scientists have been trying to create 'magic bullets'; drugs that automatically find their way to the tumour when injected into the body, and consequently focus on killing malicious cells, while not bothering with ordinary and harmless cells.