Gleevec: the “wonder drug”
Gleevec is a wonder drug because in the 90s, it became one of the first drugs to be a targeted cancer cell therapy. Chemotherapy works on mutated cells as well as normal cells which is not very effective because you need normal cells to do bodily functions. Common side effects of traditional chemotherapy is fatigue, hair loss, nausea and vomiting, pain, constipation and much more. Gleevec works because research scientist in the 70s figured out what was causing the cancerous disease and in the 90s figured out what actual gene was mutated and what caused the mutated protein. The solution was to develop a small molecule inhibitor that would work to target the cancerous cells but not the normally dividing cells. Gleevec works because it inhibits Bcr-abl semi competitively by blocking the substrate binding which is ATP. If ATP is unable to bind, then the gene cannot be phosphorylated and damage the body. It also works to change the conformation of the protein which inevitable leads to a change in the catalytic activity. A huge point of emphasis in cellular and molecular biology is that the shape of the molecule affects the function and by messing with the structure and shape of the protein, it was able to work effectively in targeting cancerous cells. While Gleevec is considered a wonder drug, there are now 2nd generation inhibitors because people were becoming resistant to the drug. The resistance was caused by point mutations in the bcr-abl kinase that allowed for increased activity in bcr-abl and decreased effectiveness of the gleevec drug.