First '3D movie' of tumour protein gives new drug hope CANCER RESEARCH UK scientists have created the first complete model of a molecule which captains a key cell signalling network to prevent cancer - and exposed the secret of how a highly selective drug can intervene to control its activity, according to a study published in PLoS Biology.
CANCER RESEARCH UK scientists have created the first complete model of a molecule which captains a key cell signalling network to prevent cancer - and exposed the secret of how a highly selective drug can intervene to control its activity, according to a study published in PLoS Biology.
Scientists based at Cancer Research UK's London Research Institute used a combination of an imaging technique and modelling to create a 3D interactive model of the enzyme protein kinase B (PKB), and observed how it functions in cells.
PKB is a chief regulator of the signalling pathways that control how cells behave. Disruption to this network is one route to cancer and excessive activation of PKB is observed in tumours. Understanding more about how PKB functions, will help scientists find out how existing drugs work to switch PKB off so that it behaves as it should in normal cells. This will help scientists develop more effective drugs to target PKB and knock out cancer.
The moving interactive model exposed a secret cavity in the enzyme's structure which was shown by the scientists to be the point where it interacts with regulatory drugs. They demonstrated that an inhibitor molecule could bind to this cavity area to lock the enzyme into an inactive state.