The official MedZine Blog

Also this week MedZine brings you the latest medical news on various medical specialisms. In this editorial two striking studies are highlighted that have implications for drug development. The first study identifies the localization of COX-2 which opens the way to the development of saver arthritis treatment. The second shows the development of a method to evaluate if drugs reach their target molecule.

Revealing to localization of COX-2 can lead to improved arthritis treatment

Arthritis drugs have been associated with increased risk of heart attack and stroke. These side effects have been attributed to their effect on COX-2. COX-2 was thought to be present in blood vessel where it is essential to preventing cloth formation. A study by Amstrong and colleagues published in PLoS One shows this model to be incorrect. The actual localization of COX-2 in the endothelium was controversial. Therefore the researchers used mice whose COX-2 gene had been replaced with luciferase, which gives fireflies their distinctive glow. This allowed researchers to create detailed images of the distribution of COX-2 throughout the body. They found that COX-2 is largely absent from the major blood vessels and instead found in the brain, gut, kidney and thymus. This knowledge can be used now to develop better drugs for arthritis and cancer with fewer side effects. 

Detecting if a drug reaches its target molecule

Drug efficacy depends on the extent of binding to a cellular target. Adverse effects are caused by binding to other components in de cell or by excessive binding to the target. In the process of drug development and testing this is a step that is almost impossible to monitor, because effects of effective drug concentration and protein conformation are difficult to analyze with in vitro affinity studies. Martinez Molina and colleagues have developed a new method to detect the extent to which drugs reach their targets in the cell and published these findings in Science. The Cellular Thermal Shift Assay (CETSA) utilizes the concept that target proteins usually get stabilized when drug molecules bind. CETSA will help to improve the efficiency of many drugs and contribute to better drug molecules and more successful treatments. In addition, the researchers examined the development of drug resistance in cells. Because CETSA can determine whether existing drugs are suitable for individual patients, the method could also be valuable to the field of personalized medicine.

Sources: Eurekalert, PLoS One and Science