Pharmacology of Anthracycline DNA Binding Agents

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Questions and Answers

What is the mechanism of action of receptor tyrosine kinase inhibitors such as imatinib?

  • They bind to docking sites for downstream signaling proteins
  • They inhibit the conversion of testosterone to estradiol
  • They bind to tyrosine residues and prevent phosphorylation
  • They bind to ATP binding sites and prevent phosphorylation (correct)

What is the common cancer mutation that leads to constitutive phosphorylation and signaling?

  • Mutation in the estrogen receptor
  • Mutation in the tyrosine residues
  • Mutation in the ATP binding site
  • Mutation in the receptor tyrosine kinase (correct)

What is the therapeutic priority in breast cancers that express estrogen receptors?

  • Inhibition of receptor tyrosine kinase
  • Reduction of estrogen production (correct)
  • Reduction of testosterone production
  • Inhibition of downstream signaling proteins

What is the mechanism of action of aromatase inhibitors such as anastrozole and letrozole?

<p>They inhibit the conversion of testosterone to estradiol (C)</p> Signup and view all the answers

What is the mechanism of action of selective estrogen receptor modulators (SERMs) such as tamoxifen?

<p>They bind to estrogen receptors and antagonize estrogen (C)</p> Signup and view all the answers

What is the mechanism of action of selective estrogen receptor downregulators (SERDs) such as fulvestrant?

<p>They cause degradation of the estrogen receptor (D)</p> Signup and view all the answers

What is the mechanism of action of anthracyclines, such as doxorubicin, on DNA?

<p>They intercalate between DNA strands, inhibiting DNA repair and leading to fragmentation and apoptosis (B)</p> Signup and view all the answers

Which of the following is a common side effect of anthracyclines?

<p>Cardiotoxicity (B)</p> Signup and view all the answers

What is the mechanism of action of microtubular inhibitors, such as vincristine and vinblastine?

<p>They bind to beta tubulin and inhibit polymerisation into microtubules (B)</p> Signup and view all the answers

What is the effect of taxanes, such as paclitaxel, on microtubules?

<p>They antagonise depolymerisation of microtubules, halting mitosis (B)</p> Signup and view all the answers

What is the common side effect of taxanes, such as paclitaxel, that requires pre-treatment with antihistamines or corticosteroids?

<p>Hypersensitivity (D)</p> Signup and view all the answers

Which of the following is NOT a type of microtubular inhibitor?

<p>Topoisomerase inhibitors (C)</p> Signup and view all the answers

What is the primary mechanism of action of alkylating agents like cyclophosphamide?

<p>Formation of covalent cross-links between nucleotide bases (A)</p> Signup and view all the answers

What is a common side effect of platinum-based compounds like cisplatin?

<p>Nephrotoxicity (B)</p> Signup and view all the answers

Which type of anticancer drug works by mimicking essential structures within the cell?

<p>Antimetabolites (A)</p> Signup and view all the answers

What is the primary advantage of using regimens of more than one drug?

<p>Improved cell cytotoxicity and reduced development of resistance (B)</p> Signup and view all the answers

Why are alkylating agents often used in combination with other drugs?

<p>They are less specific and require combination therapy (C)</p> Signup and view all the answers

What is the mode of administration of cyclophosphamide?

<p>Either oral or IV (B)</p> Signup and view all the answers

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