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yr 2 Cancer > Cancer Chemotherapy > Flashcards

Cancer Chemotherapy Flashcards

1
Q

What type of medication targets Proliferation Signalling

A

EGFR inhibitors

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2
Q

What type of medication targets Evading growth suppressors

A

Cyclin-Dependent kinase inhibitors

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3
Q

What type of medication targets Enabling Replicative immortality

A

Telomerase Inhibitors

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4
Q

What type of medication targets Inducing angiogenesis

A

Inhibitors of VEGF signalling

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5
Q

What type of medication targets Genome instability and Mutation

A

PARP inhibitors

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6
Q

What type of medication targets Resisting cell death

A

Proapoptotic BH3 mimetic

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7
Q

What do Anti-mitotics target?

A

Targets microtubules

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8
Q

What are microtubules formed of?

A

alpha and beta tubulin dimers

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9
Q

How do anti-mitotics target microtubules?

A

Disrupt assembly- Bind to free alpha-beta tubulin dimers
or
disrupt disassembly- stabilises microtubules and prevents cell division

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10
Q

Give an example of a disrupting assembly anti-mitotic

A

Vinblastine- amine protonated
vincristine- amide not protonated - slightly more potent

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11
Q

Give an example of a disrupting DISassembly anti-mitotic

A

Paclitaxel- most common
or
Docetaxel- more soluble

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12
Q

How can resistance be developed for anti-mitotics?

A

Overexpression of p-glycoproteins
Mutations in tubulin gene

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13
Q

What is an anti-metabolite?

A

An analogue of precursors for macromolecules
They inhibit essential enzymes

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14
Q

How does poisoning Thymidylate synthesis work?

A

5Fu -> FDUMP inhibits dUMP -> dTMP
Poisons enzyme
Michael addition
Causes DNA damage

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15
Q

What is an Alkylator?

A

Nitrogen mustards

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16
Q

How do alkylators work?

A

Crosslink DNA- Prevents DNA polymerase from separating strands.
Crosslink between N7 of Guanine (interstrand crosslink)

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17
Q

What chemical group is reactive on an alkylator?

A

The highly reactive aziridinium ion (N containing three membered ring)

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18
Q

Give an example of an Alkyl nitrogen mustard

A

melphalan (L-PAM)
Chlorambucil
cyclophosphamide (prodrug)

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19
Q

How are aniline mustards better?

A

Less side effects due to Lone pair on N delocalised into ring

20
Q

Explain how cyclophosphamide is a good drug (nitrogen mustard)

A

Prodrug
Not active in body- has to be activated- less TOXICITY
Has to be activated by cytochrome P450

21
Q

How can resistance be developed in relation to Nitrogen Mustards?

A

Increased expression of glutathione-S-transferase & levels of glutathione (thiol will substitute with triangle N group)
Can administer glutathione-S-transferase inhibitors^
Increased expression of excision repair enzymes
Changes in drug repair

22
Q

What are DNA platinating agents?

A

Cisplatin anti-tumour drug

23
Q

What chemical changes happen to cisplatin in the body?

A

the 2 chlorine groups are displaced with water (OH groups in turn)

24
Q

How do platinating agents work? suspectedly….

A

Inhibit DNA Polymerase
Target N7 Guanine

25
Q

How can resistance develop for DNA platinating agents?

A

Increase repair mechanism for intrastrand crosslinks (on same strand)
over expression of glutathione

26
Q

How do Topoisomerase inhibitors work?

A

Intercalate into DNA, causes shape of helix to change- therefore enzymes cant process DNA well- Prevents cell replication and causes cell death
Prevents topoisomerase from fixing double strand break

27
Q

examples of DNA intercalators (anthracyclines)

A

Doxorubicin
Daunorubicin

28
Q

How do anthracyclines work

A

Amino sugar sits in minor groove of DNA
Planar aromatic structure fit into DNA
3 rings, 2 aromatic, middle has 2 c=o which are parallel

29
Q

Whats the difference between DNA topoisomerase 1 and 2?

A

Topo 1 cuts 1 strand
Topo 2 cuts 2 strands- also fixes double strand break

30
Q

What do anthracyclines do in relation to Topoisomerases?

A

Inhibits topo 2 by preventing the fix of a double strand break

31
Q

What are the modern approaches to chemo

A

PARP inhibitors
Tyrosine Kinase Inhibitors

32
Q

How do PARP inhibitors work

A

Inhibits PARP (Poly ADP ribose polymerase)
which fixes single strand breaks caused by topoisomerase 1
leads to cell death as fix is prevented and double strand break may occur instead.

33
Q

What are the genes that are targeted by PARP inhibitors?

A

BRCA1 AND BRCA2 - Fix double strand break, if mutation than this cannot be fixed.
In healthy cells- can undergo normal homologous recombination.

34
Q

What is Olaparib?

A

BRCA PARP Inhibitor

35
Q

What are tyrosine Kinase Inhibitors?

A

NIBS- target proteins

36
Q

What are BCR and ABL?

A

2 genes- chromosome 9 and chromosome 22

37
Q

What forms the Philadelphia chromosome

A

translocation between bcr and abl (9 and 22)

38
Q

What does the Philadelphia (BCR-ABL) chromosome do?

A

Protein is always on- proliferation
Acts as a tyrosine kinase
Found in CML

39
Q

What was the first tyrosine kinase inhibitor? (BCR-ABL kinase inhibitor)

A

Imatinib

40
Q

What about Imatinib makes it a tyrosine kinase inhibitor?

A

Methyl group caused selectivity for ABL kinase
Piperidine means water soluble
2-phenylaminopyrimidine initial structure

41
Q

What does the BRAF pathway cause?

A

Cell proliferation
Gene expression
Mitosis
Differentiation

42
Q

What does a mutation in BRAF protein cause?

A

Constant signalling and activation
Causes uncontrolled cell proliferation

43
Q

What are vemurafenib , dabrafenib and sorafenib examples of?

A

BRAF inhibitors

44
Q

what are erlotinib or gefitinib

A

EGFR for NSCLC inhibits ras

45
Q

Cetuximab is for what

A

CRC blocks egfr (HER1)

46
Q

What is the mutation for Braf inhibitors

A

single mutation of V600E

yr 2 Cancer (10 decks)

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