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Medicinal chemistry > Dugga 3 - Anticancer > Flashcards

Dugga 3 - Anticancer Flashcards

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1
Q

When are cancer cells formed?

A

When normal cells lose the normal regulatory mechanisms that control growth and multiplication

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2
Q

What is a loss of differentiation?

A

When cancer cells become rogue and lose their specialised characteristics that distinguish one cell from another

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3
Q

What does neoplasm mean?

A

New growth, and is a more accurate term for cancer but not used. Tumour actually means swelling

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4
Q

What does it mean that a cancer is benign?

A

That it is localised

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5
Q

What does malignant mean?

A

When a cancer invades other parts of the body through metastasis

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6
Q

What is carcinogenesis?

A

The beginning of cancer

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7
Q

Some cancers are caused by virus, mention some

A

HPV (human papillomavirus), hepatitis B and HIV

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8
Q

What are protooncogenes?

A

Genes that normally code for proteins involved in the control of cell division and differentiation

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9
Q

What is an oncogene?

A

A protooncogene that is mutated and disrupts the normal function

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10
Q

What is the Ras protein?

A

Involved in the signalling pathway leading to cell division

Mutations of the Ras gene are present in 20-30 % of human cancers

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11
Q

What are tumour suppression genes?

A

Genes that code for proteins that are involved in these processes of checking, repair and suicide

TP53 an example and codes for the protein p53

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12
Q

Genetic defects can lead to which cellular defects?

A

Abnormal signalling pathways
insensitivity to growth inhibitory signals
Abnormalities in cell cycle regulation
Evasion of programmed cell death
Limitless cell division
Ability to develop new blood vessels
Tissue invasion and metastasis

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13
Q

What is apoptosis?

A

Programmed cell death

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14
Q

What is angiogenesis?

A

developing new blood vessels

Branching and extensions of existing capillaries

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15
Q

Do most if not all of these defects have to happen for cancer to be malignant?

Abnormal signalling pathways
insensitivity to growth inhibitory signals
Abnormalities in cell cycle regulation
Evasion of programmed cell death
Limitless cell division
Ability to develop new blood vessels
Tissue invasion and metastasis

A

Yes

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16
Q

What are integrins

A

Present on the surface of new blood vessels and absent on mature vessels. They protect new cells from apoptosis

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17
Q

Is inhibiting angiogenesis a way to tackle cancer?

A

Yes, and less toxic than traditional chemotherapy. Not used on their own but in combination with surgery, chemotherapy or radiation

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18
Q

Which other way can leaky blood vessels be targeted in battling cancer?

A

Drugs encapsulated in liposomes and nanospheres are too big to escape from normal blood vessels but will escape from leaky blood vessels and concentrate in the tumour cell

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19
Q

Why is it an issue that some tumour cells cannot receive blood supply?

A

They become dormant and cannot be reached by anticancer therapy. When cancer treatment is stopped the dormant cells start multiplying and the tumour reappers. It has been observed that such cells are more likely to metastasise

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20
Q

What is hypoxia?

A

Insufficient blood supply and lack of oxygen

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21
Q

Why is the environment around the tumour more acidic?

A

Because the lack of oxygen means that tumour cells are forced revert to glycolysis to produce energy. That leads to acidic byproducts within the cell. They export these acidic protons to the extracellular space.

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22
Q

What is a prophylactic?

A

A way of preventing disease

23
Q

What prophylactic could be used to prevent cancer in susceptible individuals

A

Angiogenesis inhibitors

24
Q

Which are important anticancer agents?

A

Agents that inhibit the polymerisation and depolymerisation of microtubules

25
Q

Give examples of what binds to tubulin and inhibit polymerisation process

A

Vinca alkaloids, podophyllotoxin, combretastatins, other natural products

26
Q

What does Paclitaxel do?

A

Bind to tubulin and accelerate polymerisation by stabilising the resulting microtubules

27
Q

What are tyrosine kinase inhibitors?

A

Selective against receptor tyrosine kinase targets which affect survival of cancer cells

28
Q

What is gefinitib?

A

A kinase inhibitor used to treat lung cancer

29
Q

Which different kinase inhibitors exist?

A

cycin-dependent kinase inhibitors (CDK)
Inhibitors of the MAPK signal transduction pathway (target B Raf)
Inhibitors of PI3K-PIP3 pathways
Janus kinase
Multi-receptor tyrosine kinase inhibitors
Inhibitors of ALK
Inhibitors of RET and KIF5B-RET

30
Q

Do cancers overexpress proteins involved in signalling pathways stimulating growth and division?

A

Yes

31
Q

Is the abnormal form of Ras associated with many cancers?

A

Yes

32
Q

What are protein kinases?

A

Enzymes using ATP to phosphorylate hydroxyl or phenol groups

33
Q

How do kinase inhibitors work?

A

Bind to the ATP binding region and other regions of the active site

34
Q

What are metalloproteinases?

A

Zinc-dependent enzymes that play an important role in invasiveness and metastasis of cancer. Catalyse cleavage of peptide bonds in protein substrates.

35
Q

What are four main groups of MMPs (matrix metalloproteinases)

A

Collagenases
Gelatinases
Stromelysins
Membrane type

36
Q

What are MMPIs? (Matrix metalloproteinase inhibitors) And how are they useful?

A

Inhibit the breakdown of extracellular matrix to make it difficult to cancers to metastasise and spread

37
Q

What are proteasome inhibitors?

A

Proteasomes eliminate damaged or misfolded proteins. Proteasomes destroy cells marked with ubiquitin. Inhibiting proteasomes in cancer cells could be useful in order to trigger apoptosis in cancer cells

38
Q

How do MMPs work (matrix metalloproteinases) and why would be be good to inhibit them?

A

Zinc-dependent enzymes degrade the extracellular matrix and encourage angiogenesis, tumour propagation and metastasis

39
Q

What are histone acetylases and deacetylases involved in?

A

Regulation of transcription

40
Q

How are monoclonal antibodies used?

A

Targeted against antigens which are overexpressed in certain cancer cells. Useful in treating breast cancer, colorectal cancer and lymphomas

41
Q

What is an antibody drug conjugate and how can it be used?

A

Linking a highly potent drug or radioisotope to an antibody. Will target specific cancer cells and drug would be released inside the cell after being enveloped

42
Q

How can drugs be attached to antibodies?

A

Via lysine residues. Or the antibody can be made to produce thiol or aldehyde groups to which the drug can be attached

43
Q

What is ADEPT?

A

An antibody-enzyme conjugate which is targeted to specific cancer cells. Once the antibody is attached to a cancer cell, a prodrug is administered which is activated by the enzyme at the tumour site

44
Q

WHat is ADAPT?

A

Antibody that has catalytic activity designed to activate a prodrug

45
Q

WHat is GDEPT?

A

The delivery of a gene to a cancer cell. The genes code for enzymes capable of activating an anticancer prodrug

46
Q
A
47
Q

Give examples of alkylating agent

A

Cisplatin. Works on nucleic acids. React with nucleophile, forms covalent bonds. Nitrogen mustard was first

48
Q

Give example of intercalation agent

A

Anthracycline
Doxirubicin
Idarubicin
Can slip into DNA and distort structure

49
Q

Give example of antimetabolite

A

Methotrexate (no severe side effects, can be used life long, can be user antibiotics)
Acts on enzymes
Similar to folic acid and inhibit formation of FH4

50
Q

Give example or hormone based

A

Prednisolone
Against hormone dependent cancers

51
Q

Give example of inhibitors of tubulin polymerisation

A

Vinblastine

52
Q

Give example of inhibitors of tubulin depolymerisation

A

Paclitaxal

53
Q

Give example of inhibitors or signaling pathway

A

Lonafarnib (Ras)

Gefitinib (protein kinase)

Medicinal chemistry (10 decks)

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