Aiding in Drug Development and Discovery

The cell is the basic structural and biological unit of all organisms. How our cells function, including if they divide or die, is tightly controlled by a large collection of proteins called kinases. When these proteins mutate and their signaling capabilities become faulty, cell growth and division can be negatively impacted and diseases such as cancer can occur.

Live cell model systems are an important tool for laboratory researchers in their quest to develop and evaluate cancer drugs against target kinases. In the past, scientists typically used biochemical methods with kinase proteins purified from ruptured cells, but this testing approach isn’t relevant to how drugs behave in the body. A useful live cell model can reflect the endogenous biology, or true-to-life conditions, observed within the human body. With the target proteins contained inside a live cell, researchers can better predict how the drug would behave in the human body. Obtaining this more predictive data in the early stages of drug exploration will allow researchers to move through research and development faster and continue to advance human health.

Promega scientists developed a unique way to study kinases using an energy transfer technique and specially designed cell-permeable detection probes that enable testing in a live cell environment. The NanoBRET® TE Intracellular Kinase Assays use Bioluminescence Resonance Energy Transfer, or BRET, to measure the binding of the drug to the kinase. This new technique helps researchers determine if the drug gets into the cell, if it interacts with the intended target, and for how long it stays bound despite other things in the cell trying to bump it off. With this new live cell approach, pharmaceutical researchers can arm themselves with the comprehensive data they need for a more complete picture of kinase target effects as they move to the next phases of development.