Gleevec a Crushing Blow to Cancer - 2893 Words

Abstract Gleevec is heralded as a savior drug for cancer research. Created by the rational drug design model, Gleevec targets the tyrosine kinase enzyme in CML patients.[10] By targeting and binding to the active sites of the cancerous cells, Gleevec denaturizes them, preventing the spread of the disease.[10] Gleevec has been FDA approved to be administered to patients diagnosed with chronic myelogenous leukemia and also patients with gastrointestinal stromal tumors.[6] Although, this treatment has also been proved to aid in other fields of medicine, ranging from treating other types of cancers to delaying tumor growth to therapy for diabetes and even to cancer treatment in pets.[5,6,8,9] However, for Gleevec to have been made other†¦show more content†¦Herceptin is a drug targeting cancerous cells in some breast cancer patients.[7] Figure 1- RituxanFigure 2- Herceptin The next goal was to find a molecule that could bind into a growth-factor receptor that was more common in cancer cells. This was done in 2001 and it had great success immediately; â€Å"Then just this year researchers at Sloan-Kettering showed that the drug could dramatically boost the effectiveness of standard colorectal-cancer chemotherapy, shrinking tumors in more than a fifth of otherwise hopeless cases.†[7] These discoveries paved the way for Gleevec to be made by rational drug design. The Invention of Gleevec â€Å"After the Philadelphia chromosome mutation and defective bcr-abl protein were discovered, the investigators screened chemical libraries to find a drug that would inhibit that protein. With high-throughput screening, they identified 2-phenylaminopyrimidine. This lead compound was then tested and modified by the introduction of methyl and benzamide groups to give it enhanced binding properties, resulting in imatinib.†[6] The composition of Gleevec is C29H31N7O and Figure 3- Imatinib Structure Nicholas Lydon, Brian Druker and Charles Sawyers are credited with the structure and invention of the drug, which they developed throughout the late 1990s.[6] The FDA approved Gleevec for use in May 2001.[6] Gleevec Targeting CML Gleevec was a drug that was invented by use of the now popular, rational