45 Questions
What is the primary consequence of alkylation on DNA synthesis?
Formation of covalent bonds between DNA strands
What is the primary effect of nitrosoureas on bone marrow?
Severe effect on replicative capacity
During which phase of the cell cycle are cells most susceptible to alkylating agents?
Late G1 and S phase
Which of the following statements is true about methotrexate?
It can be inhibited by dietary folate
What is a common side effect of platinum-based DNA synthesis inhibitors?
Lots of vomiting and nausea
What is a mechanism of action of 5-FU?
Inhibition of thymidylate synthetase
What is the primary mechanism of action of alkylating agents in cancer treatment?
Formation of covalent bonds in DNA
What is the common side effect of cyclophosphamide and methotrexate?
Bone marrow depression
What is the characteristic of platinum-based DNA synthesis inhibitors?
Water-soluble
Which of the following is not a route of administration for methotrexate?
Subcutaneous
Which type of cancer is commonly treated with platinum-based DNA synthesis inhibitors?
Solid tumours
What is the primary mechanism of action of carboplatin?
Alkylation of DNA
What is the primary mechanism of action of doxorubicin?
Inhibition of topoisomerase II
Which of the following is NOT a side effect of doxorubicin?
Diarrhea
What is the common mechanism of action of plant derivatives such as vinca alkaloids and taxanes?
Binding to microtubules
What is the effect of etoposide on the cell cycle?
Blocks cells in late S or G2 phase
Which of the following is a natural source of etoposide?
Mandrake root
What is the primary mechanism by which fluorouracil prevents DNA synthesis?
By preventing methylation of the uracil analogue
What is the effect of Fludarabine on DNA synthesis?
It is used as a substrate for DNA polymerase and inhibits its active site
What is the primary mechanism by which Cytarabine inhibits DNA synthesis?
It binds to DNA polymerase and inhibits its action
What is the primary mechanism by which cytotoxic antibiotics affect nucleic acid structures?
By modifying DNA through topoisomerase inhibition
What is a common side effect of fluorouracil and Cytarabine?
Epithelial/mucosal layer damage
What is the primary mechanism by which Penostatin inhibits DNA synthesis?
By inhibiting adenosine deaminase
Lomustine is a nitrogen mustard.
False
Methotrexate is a purine analogue.
False
Thymidylate synthetase is inhibited by 5-FU.
True
Carboplatin has more side effects compared to cisplatin.
False
Methotrexate can be administered through subcutaneous injection.
False
Intra-strand linking and crosslinking occurs between N7 & O6 of adjacent adenines.
False
Cisplatin is not used to treat solid tumours.
False
Platinum-based DNA synthesis inhibitors are highly myelotoxic.
False
Carboplatin is an oral medication.
False
The primary mechanism of action of alkylating agents is to inhibit DNA synthesis.
True
Doxorubicin inhibits topoisomerase I.
False
Vinca alkaloids target microtubules.
True
Etoposide is derived from the bark of the Pacific Yew tree.
False
Taxanes are derived from the periwinkle plant.
False
Doxorubicin is given orally.
False
Etoposide binds to the complex formed between DNA and topoisomerase.
True
Fluorouracil is a nucleoside analogue that binds to DNA polymerase and inhibits its action.
False
Cytarabine is a pyrimidine nucleoside analogue that inhibits purine metabolism.
False
Fludarabine is metabolized to a monophosphate form that inhibits active site of DNA polymerase.
False
Penostatin inhibits adenosine deaminase, leading to increased purine metabolism.
False
Cytotoxic antibiotics, such as anthracyclines, are recommended for use in combination with radiation.
False
5-FU is an analogue of 2’-deoxycytidine.
False
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
- Folate antagonists (e.g. Methotrexate)
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.
Test your knowledge of cancer development, cellular signaling, and treatment strategies. Learn how to integrate knowledge of cellular signaling in cancer development and cell death to specific drug mechanisms. Understand the principles of cancer development and describe treatment strategies.
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