Cancer Chemotherapeutic Agents Lecture 4 - Dr. M Casely-Hayford: Antimetabolites

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Which of the following enzymes is NOT essential for DNA synthesis?

DNA polymerase

Thymidylate synthase

RNA polymerase (correct)

DNA ligase

Which of the following mechanisms does NOT describe the action of antimetabolites?

Arrest of DNA chain elongation

Promotion of nucleotide incorporation into growing DNA strand

Inhibition of enzymes involved in DNA synthesis

Inhibition of RNA function (correct)

Which of the following is NOT a common side effect of antimetabolite treatment?

Gastrointestinal toxicity

Neurotoxicity (correct)

Myelosuppression

Alopecia

Which of the following B vitamins is NOT involved in DNA synthesis?

Vitamin B5 (Pantothenic acid) Signup and view all the answers

Which of the following is NOT a reason for using antimetabolites in cancer treatment?

High selectivity for cancer cells Signup and view all the answers

Which of the following is NOT a risk factor for folate deficiency?

Hyperthyroidism Signup and view all the answers

Which compound acts as a one carbon source for dTMP synthesis?

N5, N10-methylene FH4 Signup and view all the answers

Which drug is a potent inhibitor of thymidylate synthase?

Methotrexate Signup and view all the answers

Which compound is a coenzyme for essential biochemical transformations?

Folic acid Signup and view all the answers

Which drug is known for its superior pharmacokinetic properties?

Methotrexate Signup and view all the answers

Which compound is methylated by N5, N10-methylene FH4 to give dTMP?

Deoxyuridine monophosphate (dUMP) Signup and view all the answers

Which drug inhibits DHFR and depletes the cofactor N5, N10-methylene FH4?

Methotrexate Signup and view all the answers

What is the effect of depletion of the cofactor N5,N10-methylene FH4 on cellular processes?

It has the greatest effect on dTTP synthesis. Signup and view all the answers

What is the difference between aminopterine and methotrexate?

Methotrexate has a methyl group at position R, while aminopterine does not. Signup and view all the answers

What is the role of the sulfhydryl group in thymidilate synthase enzyme during dTMP synthesis?

It is involved in the formation of the ternary complex. Signup and view all the answers

What is the mechanism of action of 5-fluorouracil (5-FU)?

5-FU inhibits the activity of thymidilate synthase enzyme. Signup and view all the answers

How does the presence of the fluorine atom in 5-fluorouracil (5-FU) affect the electrophilicity of the C6 position in FdUMP?

The fluorine atom increases the electrophilicity of the C6 position. Signup and view all the answers

What is the effect of abstraction of a C5-H by the N10 in the co-factor (Step 4 above) in the fluorinated ternary complex?

It is not possible in the fluorinated ternary complex. Signup and view all the answers

What is the effect of the absence of dTMP on cellular processes?

It blocks DNA synthesis leading to cell death. Signup and view all the answers

What makes 5-FU a particularly useful drug for the treatment of skin cancers?

It shows a high level of selectivity for cancer cells over normal skin cells. Signup and view all the answers

What is the role of the cofactor N5,N10-methylene FH4 in the normal synthesis of dTMP?

It acts as a source of carbon atoms in the reaction. Signup and view all the answers

What is the difference between deoxyuridine monophosphate (dUMP) and fluorinated deoxyuridine monophosphate (FdUMP)?

FdUMP has a fluorine atom at the C6 position, while dUMP does not. Signup and view all the answers

Cancer Chemotherapeutic Agents Lecture 4 - Dr. M Casely-Hayford: Antimetabolites

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Questions and Answers

Which of the following enzymes is NOT essential for DNA synthesis?

Which of the following mechanisms does NOT describe the action of antimetabolites?

Which of the following is NOT a common side effect of antimetabolite treatment?

Which of the following B vitamins is NOT involved in DNA synthesis?

Which of the following is NOT a reason for using antimetabolites in cancer treatment?

Which of the following is NOT a risk factor for folate deficiency?

Which compound acts as a one carbon source for dTMP synthesis?

Which drug is a potent inhibitor of thymidylate synthase?

Which compound is a coenzyme for essential biochemical transformations?

Which drug is known for its superior pharmacokinetic properties?

Which compound is methylated by N5, N10-methylene FH4 to give dTMP?

Which drug inhibits DHFR and depletes the cofactor N5, N10-methylene FH4?

What is the effect of depletion of the cofactor N5,N10-methylene FH4 on cellular processes?

What is the difference between aminopterine and methotrexate?

What is the role of the sulfhydryl group in thymidilate synthase enzyme during dTMP synthesis?

What is the mechanism of action of 5-fluorouracil (5-FU)?

How does the presence of the fluorine atom in 5-fluorouracil (5-FU) affect the electrophilicity of the C6 position in FdUMP?

What is the effect of abstraction of a C5-H by the N10 in the co-factor (Step 4 above) in the fluorinated ternary complex?

What is the effect of the absence of dTMP on cellular processes?

What makes 5-FU a particularly useful drug for the treatment of skin cancers?

What is the role of the cofactor N5,N10-methylene FH4 in the normal synthesis of dTMP?

What is the difference between deoxyuridine monophosphate (dUMP) and fluorinated deoxyuridine monophosphate (FdUMP)?

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