Antieoplastic agents Flashcards by tcarlso 3

What are carcinomas?

Malignant cells that arise from epithelial tissues (ectoderm or endoderm)

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What are Sarcomas?

Malignant cells that arise from CT (mesoderm)

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What are neoplasms that involve the bone marrow and peripheral blood called?

Leukemias

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What are neoplasms that arise from B or T lymphocytes, and commonly present as masses within lymph nodes or othe soft tissues?

Lymphomas

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What are myelomas?

Plasma cell diseases

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What is the role of p53?

intracellular signal that induces apoptosis

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What is the mutation in tumors that allows for sustained proliferation?

Telomerase

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What are the enzymes that allow tumors to metastisize?

metalloproteases

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What are the five main types of lymphoid malignancies?

Acute lymphoid leukemia
Chronic lymphoid leukemia
non-Hodgkines
Hodgkins
Plasma cell diseases

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What is the philidelphia chromosome? What disease does this cause?

Translocation between chromosome 9 and 22, causing a fusion of the BCR-ABL genes

Chronic myeloid leukemia

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What is the purpose of the ABL gene?

Makes a Y kinase that stimulates cellular growth

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What are the common changes that protooncogenes undergo to facilitate cellular growth? (3)

Constitutive activity
Resist degradation
Increase expression

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What is the Ras/Raf kinase cascade used for, generally?

Growth signal

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What is the receptor in breast CA that trastuzima inhibits?

Her2/neu

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What is curative intent when describing antineoplastic drugs?

Drugs that are used to cure CA

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What does it mean for a drug to be an adjuvant therapy?

Drug that is used to decrease the changes that a CA will return

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What does it mean for a drug to be a neo-adjuvant therapy?

Drug that is used to shrink the tumor before primary treatment

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True or false: ras is mutated in about 30% of all cancers

True

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c-myc is upregulated in what types of CA?

Colorectal cancers

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What is Hodgkin’s lymphoma?

B cell CA

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Mutations in the IGF pathway lead to what?

Prostate, breast, and colorectal CA

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What are the three major points in the cell cycle, where there are checkpoitns?

G1/S
G2/M
metaphase/anaphase

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What are the two things that are checked at the G2/M checkpoint?

Is all DNA intact

Are all chromosomes attached to the mitotic spindle

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What is the thing that is checked at the G2/M check point?

Is the DNA completely replicated

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What are the two things that are checked at the G1/S check point?

Cell size/nutrition good? | DNA intact?

What is the general target of chemotherapy?

Highly proliferative cells

Is the therapeudic index high or low with chemo?

Low

True or false: in general, the longer the cell doubling time of the tumor, the easier it is to treat

False- the shorter the doubling time

Why do we use combinatiion therapies?

Avoid evolution/selection of the tumor cell

What is the cell kill hypothesis?

Chemo kills via first order kinetics

Since chemo kills via first order kinetics, there must be repeated doses of a drug. What is the limit to these doses?

Adverse side effects

Why a tumor cells fast to evolve?

Really unstable DNA

What is the specific protein that, when upregulated in a tumor cell, allows it to survive?

MDR transporter

Why don't all cells within a tumor die at the same rate?

Not all have equal acess to blood supply

Most chemotherapeutic drugs ultimately kill cell through what mechanism?

Inducing apoptosis

What is epithelial-mesenchymal transition?

The process by which cells lose adhesive properties and become motile

What is the basis for the immune suppression with chemo?

Bone marrow toxicity since it divides a lot

What is the basis for the GI issues seen with chemo?

Attack of fast replicating enterocytes

What are the four ways of perturbing normal DNA synthesis in cancer cells?

1. Staving pyrimidine/purines 2. Incorporation of altered nucleotides 3. Alkylating, crosslinking etc of DNA 4. Prevent topoisomersase

What are the two ways of perturbing mitosis?

Prevent micotrubule formation Prevent microtule destruction

What are the three targeted ways of killing tumors?

1. Pertubing hormone/growth signaling 2. Inhibiting blood supply 3. Target activating proteins

What part of the cell cycle do DNA alkylating drugs and intercalating drug act?

non specfic (all of them)

True or false: Drugs that are nonspecific are still going to kill replicating cells more often than slower replicating ones

True

What are the two purines?

Adenosine | Guanine

What are the three pyrimidines?

Thymidine Cytiding Uridine

What are nucleosides?

Nucleobases with a ribose attached

What are nucleotides?

Nucleobases with a ribose and a phosphate

What is the main process that antimetabolites target?

De novo nucleotide biosynthesis

What, generally, are the molecules that make up the antimetabolites?

analogs of purines and pyrimidines

What part of the cell cylce do antimetabolites generally work?

S phase

What is the role of ribonucleotide reductase?

Turns ribonucleotides into deoxyibonucleotides

What is the precursor for purines?

inosine monophosphate

What is the MOA of methotrexate? (hint, two enzymes involved)

Blocks dihydrofolate reductase from forming THF, which inhibits thymidylate synthase, which decreases dTMP production

Which cancers are methotrexate particularly useful in treating?

Acute lymphoblastic leukemia Osteosarcomas Choriocarcinomas

How can you deliver a high dose of methotrexate? MOA?

administer leucovorin, which prevent toxicity via THF derived cofactors

What is the MOA of resistance of tumor cells to methotrexate?

Impair transport | Change/elevate DHFR

What are the adverse effects of methotrexate?

Bone marrow suppression Nephrotoxicities Hepatic dysfunction

What is the MOA of 5FU?

fdUMP causes DNA/RNA damage by decreasing thymidylate levels

What is the enzymes that 5FU inhibits?

Thymidylate synthetase

What are the uses of 5FU?

GI cancers | Part of breast treament

What are the adverse effects of 5FU?

Oral and GI ulcers | Bone marrow suppression

What is the MOA of resistance to 5FU?

Amplification of thymidylate synthetase

What is capecitabine?

Prodrug of 5FU

What is the MOA of cytarabine (Ara-c)?

Ara-c is converted by deoxycytidine kinase,

What are the cancers that cytarabine is used to treat?

Leukemias/hematological tumors

What is the enzyme in celll that breaks down cytarabine (ara-c)? What part of the body does not have very much of this enzyme?

Cytidine deaminase | CNS

What phase of the cell cycle does cytarabine act in?

S phase

What are the adverse effects of cytarabine?

Cerebellar syndrome (dysarthria, nystagmus, ataxia) Renal/hepatic dysfunctino

What drug causes cerebellar syndrome? Why?

Cytarabine d/t lack of cytadine deaminase in the CNS

Antieoplastic agents Flashcards

(69 cards)