Millipore Technical Publications |
 | AN- 1715-0706 White Paper | |
White Paper: Battle at the Gates: Combating Mutant Kinases | ||
| Lit No: | 1715-0706 | |
| Year: | 2006 | |
| White Paper Molecular therapeutics that target protein kinases represent a major advance in the treatment of disease, particularly cancer. These drugs have proven successful in treating some cancer patients, particularly those with pathologies derived by oncogenic forms of tyrosine kinases. One of the first successful drugs developed against protein kinases is Gleevec® (imatinib), which inhibits the Abl and Kit tyrosine kinases. The initial success of Gleevec was tempered by patients who had responded initially to the drug but subsequently developed clinical resistance. The molecular basis of this resistance was soon identified—patients were shown to possess previously undetected mutant forms of Abl and Kit. Shortly thereafter during clinical studies of the EGF receptor (EGFR) inhibitors Iressa® (gefitinib) and Tarceva® (erlotinib), a similar phenomenon was observed, and mutant forms of EGFR resistant to the inhibitors were identified. Click the PDF above for the full document. | |
| |
| |