Gleevac Essay Example | Topics and Well Written Essays - 3000 words

Gleevac - Essay ExampleIt has four pKa values 1.52, 2.56, 3.73, 8.07, very soluble in buffers of PH 5.5 and slightly soluble in neutral/alkaline aqueous buffers. Gleevec recognizes the auto inhibitory conformation of the activation loop of the protein that regulates the kinase application. The structure of inactive state is distinct between different kinases. It has a half-life of 15 hours and allows periodic administration.Gleevec is used to treat the chronic phase of CML though applications have been found in Advanced and blast crisis phases. Its efficacy has been found to reduce with phase progression.Most patients that seizet respond to gleevec are in advanced stages of CML at the initiation of treatment. Failure rate of imatinib in patient with chronic phase CML remains low(at slight than 15%at 18 months) in patients who did not respond to interferon.In the 1980s and 90s much skepticism prevailed first on the exploitation of compounds with specificity among protein kinases . Secondly, the targeting of singular molecular defects seemed insufficient in the treatment of highly heterogeneous cancer 11. Gazit in 1989 reported low molecular weight tyrosine kinase inhibitors with selective activity towards EGFR. These inhibitors were called tyrophostins. Tyrophostins were useful in selective antiproliferation agents for proliferative diseases caused by hyperactivity of protein tyrosine kinases. Though tyrophostins were not clinically developed, they provided the proof of the principle of selective inhibition of tyrosine kinases by using small molecules 16. after 2 phenylaminopyrimidines were reported as selective inhibitors for protein kinases C (PKC), Abelson (ABL) and platelet derived growth factor receptor (PDGFR) kinases 3. Tyrosine kinases mediate many of the signaling pathways by which cancer cells agitate their proliferation and survival. They control cellular function and are thought to be too similar to be inhibited in-vivo 15. Overall imatinib sho ws