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BMSC2210 - Chemotherapy > L14 - Anti-cancer 2: Targeting DNA replication, transcription & cell division > Flashcards

L14 - Anti-cancer 2: Targeting DNA replication, transcription & cell division Flashcards

1
Q

Aims of palliative chemotherapy?

A

extend survival but patient will eventually die

symptoms recur between treatments

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2
Q

Aims of curative chemotherapy for solid tumours?

A

tumour reduced by surgery/radiation

treatment of micrometastases continued

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3
Q

Aims of curative chemotherapy for disseminated cancers?

A

combination drug therapy (reduce drug resistance)

each drug has different cellular site of action

each drug has diff. organ toxicity

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4
Q

How is the cell cycle different in cancer cells?

A

cancer cells go through cell cycle much faster

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5
Q

What are antimetabolites?

A

structurally related to normal compounds

inhibit/interfere with DNA/RNA synthesis

S-phase specific

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6
Q

What is MTX structurally related to?

A

folic acid

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7
Q

What is methotrexate (MTX)?

A

antimetabolite

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8
Q

What is MTX retained in cells as?

A

MTX-polyglutamate compounds

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9
Q

How can MTX be rescued?

A

Leucovorin - produces tetrahydrofolate in cells

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10
Q

Where does MTX target?

A

cells in S phase

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11
Q

What cancers is MTX used against?

A

ALL
Breast
Head and neck

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12
Q

How does MTX work?

A

inhibits dihydrofolate reductase (DHFR) and stops production of tetrahydrofolate - stops production of precursors for DNA synthesis

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13
Q

What does DHFR usually do?

A

catalyses folate into tetraphydrofolate - used for synthesis of precursors of DNA synthesis

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14
Q

Is MTX toxic?

A

potentially - may block stem cell replication

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15
Q

Can MTX treat other diseases?

A

Yes - low dose treatment of rheumatoid arthritis

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16
Q

How is MTX administered?

A

oral
IV
IM
intrathecally

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17
Q

What is the fate of MTX?

A

unchanged drug appears in urine

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18
Q

What is 6-mercaptopurine?

A

nucleotide anlogue

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19
Q

What does 6-Mercaptopurine do?

A

inhibits purine biosynthesis

converted into thio-IMP by HGPRT

blocks synthesis of other nucelotide precursors

blocks phospho-ribosylamine synthesis

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20
Q

How does 6-Mercaptopurine lead to non-functional molecules?

A

incorporated into DNA and RNA

ribosomes cannot translate chemically modified RNA

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21
Q

How is there resistance to 6-Mercaptopurine?

A

inherited mutations - do not make HGPRT

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22
Q

What is 5Fluorouracil (5FU)?

A

uracil analogue

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23
Q

What does 5FU do?

A

block production of dTMP by thymidylate synthetase, needed for DNA synthesis and cell growth

deplete intracellular nucleotide pools

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24
Q

What is 5FU often given in combo with?

A

MTX

they target diff enzymes - 2 diff aspects of DNA and RNA synthesis in cancer cells

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25
Q

What is Gemcitabine?

A

analogue of deoxycytidine

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26
Q

What does Gemcitabine do?

A

inhibit DNA synthesis

can be phosphorylated

deaminated to non-toxic products & excreted in urine

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27
Q

What is Gemcitabine used to treat?

A

advanced metastatic pancreatic cancer

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28
Q

how is Gemcitabine administered?

A

infused IV

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29
Q

Side effects of Gemcitabine?

A

myelosuppression

depressed WBC count

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30
Q

What is Cytarabine (cytosine arabinoside/AraC)?

A

chain terminator of DNA synthesis

inhibit DNA polymerases

competes with normal deoxyribose precursors

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31
Q

side effects of Cytarabine

A

myelosuppression

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32
Q

Fate of cytarabine?

A

excreted in urine

33
Q

What does Dactinomycin do?

A

binds to DNA minor groove -

interferes with transcription AND DNA replication

DNA double strand breaks

34
Q

What is dactinomycin used in combination with?

A

MTX

35
Q

Why is there resistance to dactinomycin?

A

P-glycoprotein - major mediator against cancer drugs

36
Q

why is the double strand break system of dactinomycin not that effective?

A

enzyme system repairs breaks

37
Q

Why are antibiotics used as cancer therapy?

A

to block the life of cancer cells

38
Q

Fate of dactinomycin?

A

urine and bile

doesn’t cross blood-brain barrier

39
Q

What are the 2 anthracyclines?

A

Doxorubicin

Daunorubicin

40
Q

How do anthracyclines work?

A

intercalate into DNA

generate free radicals - break up DNA strands

interfere with DNA breakage repair system - apoptosis can be activated

oxidise lipids in membranes

41
Q

What cell cycle stage to anthracyclines target?

A

S and G2 phase

42
Q

What are anthracyclines used to treat?

A

breast
lung
leukaemia

(in combo)

43
Q

What is the fate of anthracyclines?

A

bile and urine

44
Q

What do alkylating agents do?

A

transfer alkyl groups to DNA

act on adjacent G bases in DNA

45
Q

What type of cells do alkylating agents target?

A

rapidly dividing cells

46
Q

What do alkylating agents need for transformation into active drug?

A

cytochrome p450 - hydroxylates and activate

47
Q

What are alkylating agents used to treat?

A

solid and lymphatic tumours

48
Q

original use of alkylating agents?

A

mutagens to create mutations in organisms

49
Q

Why can alkylating agents be used for brain cancer?

A

cross blood-brain barrier

50
Q

2 examples of alkylating agents?

A

Temozolomide

Decarbazine

51
Q

How are aklylating agents administered?

A

orally (temozolomide)

IV (decarbazine)

52
Q

What are platinum coordination complexes?

A

cisplatin
carboplatin
oxaliplatin

53
Q

How do platinum coordination complexes work?

A

form intra- and inter-strand crosslinks

interferes with transcription AND DNA replication

54
Q

What cell cycle stage to platinum coordination complexes target?

A

G1 and S phase

55
Q

What does cisplatin treat?

A

solid tumours

testicular (VBL and bleomycin combination)
bladder

56
Q

What are topoisomerase I inhibitors?

A

bind to enzyme-DNA intermediate and prevent re-ligation of DNA strand by Topo I

57
Q

What are the topoisomerase I inhibitors?

A

Topetecan

Irinotecan

58
Q

What is Topetecan used to treat?

A

metastatic ovarian cancer

lung cancer

59
Q

What is Irinotecan used to treat?

A

Colon & rectal cancer (combo with 5FU and leucovorin)

60
Q

How are Topo I inhibitors administered?

A

IV

61
Q

What does Topo II usually do?

A

breaks and reseals DNA strands

62
Q

What are Topo II inhibitors?

A

Daunorubicin
Doxorubicin

Etoposide
teniposide

63
Q

What do Etoposide and teniposide do?

A

bind to transient cleavable form of enzyme-DNA complex = double strand breaks

64
Q

How are daunorubicin and Doxorubicin Topo II inhibitors

A

intercalate DNA

prevent topo II catalysed breakage/reuinion - DNA strands NOT repaired

65
Q

What cell cycle stage do topo Inhibitors target?

A

S phase

66
Q

What is Etoposide used to treat?

A

testicular cancer

bleomycin, cisplatin

67
Q

What is teniposide used to treat?

A

ALL
gliomas
neuroblastomas

68
Q

How are topo II inhibitors administered?

A

IV and oral

69
Q

What do Vinca alkaloids do?

A

block mitosis in METAPHASE

bind to tubulin - inhibit microtubule formation

induce spindle dysfunction

70
Q

What do taxanes do?

A

block mitosis in METAPHASE

bind b-tubulin subunit

promote polymerisation BUT microtubules are non-functional and “frozen”

71
Q

What are the 2 Vinca alkaloids?

A

Vincristine (VX)

Vinblastine (VBL)

72
Q

What are vinca alkaloids isolated from?

A

Vinca rosea

73
Q

Side effects of VX?

A

neurotoxic

74
Q

Side effects of VBL?

A

myelosuppressant

75
Q

What are Vinka alkaloids used to treat?

A

rapidly dividing tumours

76
Q

What are the 2 taxanes?

A

Paclitaxel

Docetaxel

77
Q

What are taxanes used to treat?

A

advanced ovarin & breast cancers

non-small cell lung

78
Q

Side effect of taxanes?

A

neutropenia

79
Q

What can help reduce neutropenia from taxane treatment?

A

Filgrastim

BMSC2210 - Chemotherapy (17 decks)

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