Cancer Development and Treatment Strategies
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Questions and Answers

What is the primary consequence of alkylation on DNA synthesis?

  • Inhibition of topoisomerase
  • Stimulation of DNA transcription
  • Induction of DNA repair mechanisms
  • Formation of covalent bonds between DNA strands (correct)

    • What is the primary effect of nitrosoureas on bone marrow?

  • Enhanced differentiation of stem cells
  • Severe effect on replicative capacity (correct)
  • Stimulation of replicative capacity
  • No effect on replicative capacity

    • During which phase of the cell cycle are cells most susceptible to alkylating agents?

  • Late G1 and S phase (correct)
  • M phase
  • G2 phase
  • Early G1 phase

    • Which of the following statements is true about methotrexate?

    <p>It can be inhibited by dietary folate</p> Signup and view all the answers

    What is a common side effect of platinum-based DNA synthesis inhibitors?

    <p>Lots of vomiting and nausea</p> Signup and view all the answers

    What is a mechanism of action of 5-FU?

    <p>Inhibition of thymidylate synthetase</p> Signup and view all the answers

    What is the primary mechanism of action of alkylating agents in cancer treatment?

    <p>Formation of covalent bonds in DNA</p> Signup and view all the answers

    What is the common side effect of cyclophosphamide and methotrexate?

    <p>Bone marrow depression</p> Signup and view all the answers

    What is the characteristic of platinum-based DNA synthesis inhibitors?

    <p>Water-soluble</p> Signup and view all the answers

    Which of the following is not a route of administration for methotrexate?

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

    Which type of cancer is commonly treated with platinum-based DNA synthesis inhibitors?

    <p>Solid tumours</p> Signup and view all the answers

    What is the primary mechanism of action of carboplatin?

    <p>Alkylation of DNA</p> Signup and view all the answers

    What is the primary mechanism of action of doxorubicin?

    <p>Inhibition of topoisomerase II</p> Signup and view all the answers

    Which of the following is NOT a side effect of doxorubicin?

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

    What is the common mechanism of action of plant derivatives such as vinca alkaloids and taxanes?

    <p>Binding to microtubules</p> Signup and view all the answers

    What is the effect of etoposide on the cell cycle?

    <p>Blocks cells in late S or G2 phase</p> Signup and view all the answers

    Which of the following is a natural source of etoposide?

    <p>Mandrake root</p> Signup and view all the answers

    What is the primary mechanism by which fluorouracil prevents DNA synthesis?

    <p>By preventing methylation of the uracil analogue</p> Signup and view all the answers

    What is the effect of Fludarabine on DNA synthesis?

    <p>It is used as a substrate for DNA polymerase and inhibits its active site</p> Signup and view all the answers

    What is the primary mechanism by which Cytarabine inhibits DNA synthesis?

    <p>It binds to DNA polymerase and inhibits its action</p> Signup and view all the answers

    What is the primary mechanism by which cytotoxic antibiotics affect nucleic acid structures?

    <p>By modifying DNA through topoisomerase inhibition</p> Signup and view all the answers

    What is a common side effect of fluorouracil and Cytarabine?

    <p>Epithelial/mucosal layer damage</p> Signup and view all the answers

    What is the primary mechanism by which Penostatin inhibits DNA synthesis?

    <p>By inhibiting adenosine deaminase</p> Signup and view all the answers

    Lomustine is a nitrogen mustard.

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

    Methotrexate is a purine analogue.

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

    Thymidylate synthetase is inhibited by 5-FU.

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

    Carboplatin has more side effects compared to cisplatin.

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

    Methotrexate can be administered through subcutaneous injection.

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

    Intra-strand linking and crosslinking occurs between N7 & O6 of adjacent adenines.

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

    Cisplatin is not used to treat solid tumours.

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

    Platinum-based DNA synthesis inhibitors are highly myelotoxic.

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

    Carboplatin is an oral medication.

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

    The primary mechanism of action of alkylating agents is to inhibit DNA synthesis.

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

    Doxorubicin inhibits topoisomerase I.

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

    Vinca alkaloids target microtubules.

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

    Etoposide is derived from the bark of the Pacific Yew tree.

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

    Taxanes are derived from the periwinkle plant.

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

    Doxorubicin is given orally.

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

    Etoposide binds to the complex formed between DNA and topoisomerase.

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

    Fluorouracil is a nucleoside analogue that binds to DNA polymerase and inhibits its action.

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

    Cytarabine is a pyrimidine nucleoside analogue that inhibits purine metabolism.

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

    Fludarabine is metabolized to a monophosphate form that inhibits active site of DNA polymerase.

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

    Penostatin inhibits adenosine deaminase, leading to increased purine metabolism.

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

    Cytotoxic antibiotics, such as anthracyclines, are recommended for use in combination with radiation.

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

    5-FU is an analogue of 2’-deoxycytidine.

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

    Study Notes

    Cancer Development and Treatment

    • Cancer development involves the integration of cellular signaling pathways and cell death mechanisms
    • Principles of cancer development include:
      • Cellular signaling involved in cancer development and cell death
      • Specific drug mechanisms
      • Treatment strategies related to cancer development
      • Tailoring treatment strategies based on distinctive features of normal and cancerous cells

    DNA Synthesis Inhibitors

    • Inhibit one or more metabolic pathways involved in DNA synthesis
    • Types of DNA synthesis inhibitors:
      • Folate antagonists (e.g. Methotrexate)
        • Inhibit dihydrofolate reductase
        • Competitive inhibitor with higher affinity than dihydrofolate
        • Side effects: bone marrow depression, epithelial/mucosal layer damage
      • Pyrimidine analogues (e.g. 5-FU)
        • Inhibit thymidylate synthase
        • Activate DNA damage response
        • Side effects: myelotoxicity, epithelial/mucosal layer damage, nausea and vomiting
      • Purine analogues (e.g. Fludarabine)
        • Metabolized to a trisphosphate form
        • Inhibit active site of DNA polymerase
        • Side effects: myelosuppression
      • Nucleoside analogues (e.g. Cytarabine)
        • Analogue of 2'-deoxycytidine
        • Inhibit DNA polymerase
        • Side effects: bone marrow depression, epithelial/mucosal layer damage, nausea and vomiting

    DNA Damaging Agents

    • Alkylating agents:
      • Form covalent bonds in DNA, impeding replication
      • Intra-strand linking and crosslinking
      • Most susceptible in late G1 and S phase of cell cycle
      • Examples: nitrogen mustards (e.g. Cyclophosphamide), nitrosoureas (e.g. Lomustine)
    • Platinum-based agents:
      • Water-soluble
      • Slow IV or infusion
      • Used in solid tumors (e.g. testes, ovary)
      • Side effects: highly nephrotoxic, low myelotoxicity, vomiting and nausea
      • Examples: cisplatin, carboplatin, oxaloplatin

    Cytotoxic Antibiotics

    • Affect nucleic acid structures
    • Main mechanism: DNA modification
    • Examples: anthracyclines (e.g. Doxorubicin), bleomycin
    • Side effects: nausea and vomiting, loss of hair, myelosuppression, cardiotoxicity

    Plant Derivatives

    • Naturally occurring products
    • Often target microtubules
    • Types: vinca alkaloids (e.g. vinblastine), taxanes (e.g. paclitaxel), others (e.g. etoposide)
    • Side effects: myelosuppression, nausea and vomiting, alopecia, etc.

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