Sandbox Reserved 425: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 15: | Line 15: | ||
Fibroblast growth factor (FGFR) signaling, the factor that normally activates the BCR-ABL kinase, is the protein behind both tissue development and repair. The activation happens through a series of cascading signals that induce proliferation and migration in cells. Though mutations in the regulation of the FGFR tyrosine kinase family can result in malignant tumor growth [1]. The tyrosine kinase inhibitor Ponatinib has been used to bind to the mutant version of kinase BCR-ABL by the kinase's specific "DFG-out" conformation. The "DFG-out" conformation has the phenylalanine group of BCR-ABL flipped out of its hydrophobic binding site. Ponatinib is the first of its kind to be able to inhibit this specific mutation in BCR-ABL of the "DGF-out" combination [1]. | Fibroblast growth factor (FGFR) signaling, the factor that normally activates the BCR-ABL kinase, is the protein behind both tissue development and repair. The activation happens through a series of cascading signals that induce proliferation and migration in cells. Though mutations in the regulation of the FGFR tyrosine kinase family can result in malignant tumor growth [1]. The tyrosine kinase inhibitor Ponatinib has been used to bind to the mutant version of kinase BCR-ABL by the kinase's specific "DFG-out" conformation. The "DFG-out" conformation has the phenylalanine group of BCR-ABL flipped out of its hydrophobic binding site. Ponatinib is the first of its kind to be able to inhibit this specific mutation in BCR-ABL of the "DGF-out" combination [1]. | ||
The side effects of have caused Ponatinib to fall under scrutiny from the U.S. Food and Drug Administration (FDA). Ponatinib has shown to increase chances of deadly blood clotting and restenosis in both arteries and veins with a rate of about 1 in 5 patients. The drug has also shown to increase risk of heart attack and overall worsening of heart disease in patients. | The side effects of have caused Ponatinib to fall under scrutiny from the U.S. Food and Drug Administration (FDA). Ponatinib has shown to increase chances of deadly blood clotting and restenosis in both arteries and veins with a rate of about 1 in 5 patients. The drug has also shown to increase risk of heart attack and overall worsening of heart disease in patients [7]. | ||
----------'''Notes (to be removed)''' | ----------'''Notes (to be removed)''' | ||
