10 Questions
what is the mechanism of action of imantinib
competes with the ATP for the binding site at the kinase which stops the functionality of the kinase because it cant bind to ATP
what are the 3 ways in which cells deveop resistance against kinase inhibitors
mutations in the drug target, which impacts drug binding, bypass signalling, which maintains oncogenic signalling and mutations in downstream effetors which causes alterations in genes regulating the cell cycle
how can kinase inhibitor resistance be overcome?
by combining drugs - this increases potency and reduces the ability to develop drug resistance
which drugs target the apoptotic pathway?
BCL-2 inhibitors
what are the two apoptosis pathways?
extrinsic pathway and intrinsic pathway
describe the action of the extrinsic apoptosis pathway
binding to a receptor activates caspases responsible for apoptosis
describe the action of the intrinsic apoptosis pathway
BH3 mimetics bind to anti-apoptotic Bcl-2 family members, preventing them from trapping pro-apoptotic proteins like Bax/Bak. this leads to the activation of Bak/Bax and changes in the mitochondria leading to cell death.
give an example of a BH3 mimetic drug
Rituximab
how can cells become resistant to BH3 mimetics
mutations can cause BCL-2 to become resistant to BH3 mimetics, resistance can either be innate or acquired
what can PARP inhibitors be used to treat?
familial breast and ovarian cancer
Understand how Imatinib, a tyrosine kinase inhibitor, works to treat certain types of cancer. Learn about its mechanism of action and how it targets specific proteins.
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