Small molecule therapy pt 2
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Questions and Answers

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?

<p>BCL-2 inhibitors</p> Signup and view all the answers

what are the two apoptosis pathways?

<p>extrinsic pathway and intrinsic pathway</p> Signup and view all the answers

describe the action of the extrinsic apoptosis pathway

<p>binding to a receptor activates caspases responsible for apoptosis</p> Signup and view all the answers

describe the action of the intrinsic apoptosis pathway

<p>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.</p> Signup and view all the answers

give an example of a BH3 mimetic drug

<p>Rituximab</p> Signup and view all the answers

how can cells become resistant to BH3 mimetics

<p>mutations can cause BCL-2 to become resistant to BH3 mimetics, resistance can either be innate or acquired</p> Signup and view all the answers

what can PARP inhibitors be used to treat?

<p>familial breast and ovarian cancer</p> Signup and view all the answers

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