pyrimidine purine antineoplastics Flashcards

1
Q

Leflunomide

A

disrupts carbomyl phosphate –> orotic acid step in purine synthesis

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2
Q

Hydroxyurea

A

disrupts UDP –> dUDP step in purine synthesis via ribonucleotide reductase inhibition

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3
Q

5-FU

A

disrupts the dUMP–> dTMP via THF(methylene)–> DHF step via inhibition of thymidylate synthesis

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4
Q

MTX

A

disrupts DHF –> THF via dihydrofolate reductase

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5
Q

TMP

A

disrupts DHF –> THF via dihydrofolate reductase

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6
Q

pyrimethamine

A

disrupts DHF –> THF via dihydrofolate reductase

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7
Q

6-MP

A

disrupts PRPP–>IMP

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8
Q

Mycophenolate, ribarvirin

A

disrupts IMP–> GMP

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9
Q

Pyrimidine synthesis disrupters

A

Leflunomide, MTX, TMP, pyrimethamine, 5-FU

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10
Q

Purine synthesis disrupters

A

6-MP

mycophenolate, ribavirin

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11
Q

inhibits dihydroorotate dehydrogenase

A

leflunomide

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12
Q

inhibits dihydrofolate reductase in humans, bacteria, and protozoa respectively

A
  1. MTX - humans
  2. TMP - bacteria
  3. pyrimethamine - protozoa
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13
Q

prodrug is azathioprine

A

6-mercaptopurine, inhibits de novo purine synthesis

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14
Q

inhibit inosine monophosphate dehydrogenase

A

mycophenolate and ribovirin

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15
Q

inhibits ribonucleotide reductase

A

hydroxyurea

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16
Q

de novo pyrimidine synthesis requires what amino acids?

A

aspartate

17
Q

de novo purine synthesis requires what aa?

A

aspartate, glycine, glutamine, and THF

18
Q

capecitabine

A

prodrug form of 5-FU

19
Q

structural analog of para-aminobenzoic acid

A

sulfonamides

20
Q

what do sulfonamides accomplish?

A

they inhibit folic acid production in bacteria; humans do not synthesize folic acid and must get it from vitamines

21
Q

reversible inhibitor of inosine monophosphate dehydrogenase

A

mycophenolic acid: prevents IMP–> xanthine monophosphate

drug deprives rapidly proliferating B and T cells of key components of nucleic acids. drug is a immunosuppressant used to prevent graft rejection.

22
Q

carbomyl phosphate synthetase

A

I and II

CPS1: m1tochondria (urea cycle)
CPS2: cyTWOsol (de novo pyrimidine synthesis)