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Medicinal Chemistry 3 > Exam #02 (Anticancer Chemotherapeutic Agents) > Flashcards

Exam #02 (Anticancer Chemotherapeutic Agents) Flashcards

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1
Q

This term is defined as a disease characterized by a shift in the control mechanisms that govern cell survival, proliferation, and differentiation.

A

Cancer

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2
Q

What three characteristics define cells that have undergone neoplastic transformation?

Neoplasm = uncontrolled growth of abnormal tissue; tumor

A
  1. Immaturity (cells display cell surface antigens typical of young cells)
  2. Chromosomal abnormalities (amplified gene sequences and translocations)
  3. Excessive proliferation (forms tumors)
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3
Q

Why are cancer cells difficult for the immune system to recognize?

A

b/c they’re derived from normal cells expressing the same glycoproteins and therefore difficult to kill

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4
Q

Which cell type is defined as a small subpopulation of cells within the tumor that retains the ability to undergo repeated cycles of proliferation as well as to migrate to distant sites in the body?

A

tumor stem cells

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5
Q

What is the process of tumor cells migrating to distant sites in the body to colonize various organs called?

A

metastasis

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6
Q

True or False - tumor stem cells are genetically unstable?

A

True - their genetic instability leads to progressive selection of subclones that have a better chance of survival in a multicellular environment

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7
Q

True or False - cancer is the most common cause of death from disease in the US?

A

True (>500,000 deaths in 2005)

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8
Q

What % of patients initially diagnosed with cancer can be cured?

A

50%

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9
Q

Chemotherapy is able to cure _______% of all cancer patients?

A

10-15%

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10
Q

The comparative disorganized tissue architecture of tumors points towards cancer being a disease of ____________?

A

malfunctioning cells - tumors are disorganized mess of cells that grow faster than normal cells and form tumors

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11
Q

Which malignant tumor comes from epithelial tissue?

A

carcinomas (responsible for 80% of cancer-related deaths)

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12
Q

Which type of carcinoma comes from epithelial cells forming a protective cell layer?

A

squamous cell carcinoma

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13
Q

Which type of carcinoma comes from epithelial cells that are secreting substances into the ducts or cavities they line?

A

adenocarcinomas

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14
Q

Which malignant tumor comes from connective tissue?

A

sarcomas

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15
Q

Hematopoietic cancers come from cells of which (2) body systems? Give (2) examples of hematopoietic cancers?

A

froms cells of the CIRCULATORY and IMMUNE system

  1. lymphomas
  2. leukemias
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16
Q

Neuroectodermal tumors come from components of the nervous system. Name (2) examples of neuroectodermal tumors?

A
  1. glioma

2. astrocytoma

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17
Q

Name the (7) characteristics of malignant cells?

A
  1. freedom from contact inhibition
  2. secrete angiogenic factors (stimulates growth of blood vessels to support tumor)
  3. fast multipliers
  4. invasive growth
  5. relatively unaffected by immune system
  6. metastatic growth
  7. genetically labile (sloppy replication can be advantage i.e. drug resistance)
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18
Q

Most human cancers arise from carcinogens that act as mutagens, mutating normal genes that regulate homeostasis and growth into _______?

A

oncogenes

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19
Q

True or False - oncogenes can act across species?

A

True

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20
Q

True or False - oncogenes can arise in the genome of cells independently of viral infections?

A

True

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21
Q

Explain the role of tumor suppressor genes against errors in DNA synthesis and genetic damage. What happens if an error is found?

A

tumor suppressor genes check the integrity of the DNA before division.

If DNA is compromised, tumor suppressor genes initiates the cell to undergo apoptosis destroying the cell and DNA

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22
Q

True or False - apoptosis may be initiated if there is an inappropriate advance in cell cycle (loss of tumor suppressors, viral infection, oncogene activation)?

A

True

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23
Q

Name the (4) distinct components of cancer treatment/prevention?

A
  1. prevention
  2. early detection
  3. effective treatment
  4. supportive care
24
Q

The most appropriate method of Tx of cancer is determined by what 2 things?

A
  1. primary site of tumor vs metastatic sites (staging)

2. tissue of origin

25
Q

One third of cancer patients are cured with local modalities. Name (2) local modalities that are effective treatment if the tumor has not metastasized?

A
  1. surgery

2. radiation

26
Q

If the cancer has started to metastasize, what are the treatment options?

A

chemotherapy (systemic approach) along with surgery and radiation

27
Q

Is chemotherapy providing palliative or curative therapy in patients with widespread disseminated cancer?

A

palliative - temporary improvement of symptoms and quality of life

28
Q

List the order of the cell cycle (programmed sequence of events which occurs during cell division)?

A
  1. G1 phase
  2. S-phase
  3. G2 phase
  4. Mitosis
  5. G0 phase
29
Q

Which cell cycle phase does actual cell division occur in which DNA condenses to form chromosomes, microtubules form and organized into spindles, and a copy of each chromosome goes to each daughter cell?

A

Mitosis

30
Q

Which cell cycle phase involves a rapid increase in RNA synthesis and synthesis of enzymes needed for DNA synthesis?

A

G1 phase

31
Q

Which cell cycle phase involves a cell re-entering the reproductive cycle or temporarily (or permanently) becoming nonreproductive?

A

G0 phase

32
Q

Which cell cycle phase is characterized by DNA synthesis?

A

S-phase

33
Q

True or False - G2 phase consists of DNA, RNA, and protein synthesis and at the end of the phase, cell has enough material to form two complete cells?

A

False - no DNA synthesis in G2 phase - all other is correct

34
Q

Before DNA is copied, its integrity is checked. At the end of which cell cycle stage does this occur?

A

at the end of G1 phase

35
Q

Which cell cycle stage involves replication of DNA genome?

A

S phase

36
Q

Which regulator of the cell cycle halts the cycle in G1 phase in response to damaged DNA?

A

p53 transcription factor - cell can repair DNA or undergo apoptosis - either way preventing damaged DNA being passed on

37
Q

What does a mutated p53 transcription factor have to do with creating secondary cancer/tumor when giving chemotherapy?

A

Chemotherapy causes DNA damage that results in cells undergoing apoptosis. Cells with mutated p53 transcription factors may not undergo apoptosis as expected resulting in secondary cancer/tumor

38
Q

Loss of normal p53 transcription factor results in (INCREASE OR DECREASE) in expression of multiple drug resistance (MDR) gene?

A

Increase

39
Q

Name (5) common SE of chemotherapy

A
  1. bone marrow suppression
  2. mucositis & stomatitis - pain/inflammation of mucous membrane along GI tract and mouth, respectively
  3. alopecia (hair loss)
  4. nausea/vomiting
  5. tumor lysis syndrome
40
Q

What are the (4) components of tumor lysis syndrome?

A
  1. hyperkalemia
  2. hyperphosphatemia
  3. hypocalcemia
  4. hyperuricemia
41
Q

What is the main concern with bone marrow suppression from chemotherapy?

A

increases susceptibility to infection and bleeding from leukopenia, thrombocytopenia, agranulocytosis, granulocytopenia, neutropenia

42
Q

Why is it important to eradicate all cancer cells when treating cancer?

A

B/c a single cancer cell is capable of rapidly replicating until it is lethal to host

43
Q

What are the 3 phases of the gompertzian growth curve (cancer cell proliferation and mutation)?

A
  1. subclinical (10.000 cell)
  2. clinical (1,000,000,000 cells)
  3. fatal
44
Q

True or False - cancer cell tumor is initially monoclonal homogenous cells, but frequent mutations generate a heterogeneous mass of cells?

A

True

45
Q

What happens to tumor growth as tumor mass increases?

A

tumor grown slows

46
Q

In what phase of the gompertzian growth curve are rapidly growing cell populations relatively uniform and significantly sensitive to drug treatment?

A

subclinical phase

47
Q

In what phase of the gompertzian growth curve does cell growth slow and mutations occur and the need for drug combos is necessary?

A

clinical phase

48
Q

The extent to which a colorectal cancer has spread is described as its _____?

A

stage

49
Q

What are the (2) most common staging systems?

A
  1. TNM system

2. SEER system

50
Q

Which type of colorectal cancer is a cancer that has not begun to invade the wall of the colon or rectum (these preinvasive tumors are not counted in cancer statistics)?

A

in situ

51
Q

Which type of colorectal cancer is a cancer that has grown into the wall of the colon and rectum, but has not extended through the wall to invade nearby tissues?

A

local

52
Q

Which type of colorectal cancer is a cancer that has spread through the wall of the colon or rectum?

A

regional

53
Q

Which type of colorectal cancer is a cancer that has spread to other parts of the body?

A

distant

54
Q

What order kinetics does kinetics of cell kill with antineoplastic agents follow?

A

1st order kinetics (a constant FRACTION of cells are killed rather than a constant NUMBER of cells)

55
Q

What type of dosing schedule is used for cytotoxic drugs?

A

high-dose intermittent schedule so patient is given time to recover before subsequent dose

56
Q

Name (8) reasons tumors become resistant to the drugs used against them?

A
  1. high mutation rate of cancer cells
  2. lack of drug activating enzymes
  3. overproduction of drug metabolizing enzymes
  4. changes in target protein of chemotherapeutic agent (agent won’t be able to target cancer cells)
  5. faulty transport mechanisms for cytotoxic drugs
  6. actively transport drugs out of cell (MDR)
  7. increased levels of DNA repair enzymes
  8. increased levels of thio containing enzymes

Medicinal Chemistry 3 (6 decks)

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