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75 Cards in this Set

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lack normal functions for that cell type
undifferentiated
cancer cells which have
moved from the original site of growth
Metastases
Oncogenes are
derived from
normal genes that activate cell division
halt cell division
and promote cell differentiation
Tumor suppressor genes
absence of immune reactivity
anergy
Many oncogenes are
kinases
Normal genes can become oncogenes due to
1.) being made in excessive
amounts, 2.) mutated, or 3.) made at the wrong time of the cell cycle.
most important tumor suppressor gene
p53
been found defective in
most cancers including breast and prostate
p53
Mutations in the tumor suppressor genes such as __ are linked to breast
and prostate cancer.
BRCA1 and BRCA-2
It is easier to make a drug that __ than to correct
for the __.
inhibits oncogene function,
loss of a tumor suppressor gene
objective of most anticancer drugs is to
halt cell growth
Dosing often
calculated based on a
patient’s body surface area
is used to decrease side effects of nitrogen mustards
Mesna
not an anticancer drug
itself
Mesna
decreases irritation and bleeding of bladder caused by high mustard doses
Mesna
deny precursors for DNA/RNA/protein synthesis or inhibit metabolic enzymes
Antimetabolites
are sources of an enzyme that degrades
(deaminates) asparagine, an amino acid needed for protein synthesis
Asparaginase and pegasparaginase
irreversibly inhibits thymidylate synthetase to prevent synthesis of
thymidine
5-Fluorouracil
a nucleotide needed for DNA and RNA synthesis
thymidine
Often used with leucovorin
5-Fluorouracil
is a designed orally active precursor of 5-fluorouracil
Capecitabine (Xeloda)
must be converted to triphosphates to be active
Nucleoside-like drugs
cytarabine (Ara-C), gemcitabine, fludarabine (Ara-A), and nelrabine (Ara-G).
Nucleoside-like drugs
ara-G prodrug
nelrabine
an enzyme that is needed to metabolize adenosine
Adenosine deaminase
inhibited by two drugs - pentostatin and cladibine
Adenosine deaminase
are made into nucleotide precursors that block
DNA/RNA synthesis
Mercaptopurine and thioguanine
is a dihyfrofolate reductase inhibitor
Methotrexate
given in high doses
followed 12 to 24 hours later by leucovorin
Methotrexate
a reduced form of folate
leucovorin
multitargeted antifolate that inhibits both the enzymes
folypolyglumate and dihydrofolate reductase
Pemetrexed
Pemetrexed inhibits
folypolyglumate and dihydrofolate reductase
Antitumor antibiotics MOA
intercalation
Mitomycin MOA
crosslinks DNA
complex with DNA and interfere with DNA synthesis
Anthracyclines
They resemble
tetracyclines, having four fused rings
Anthracyclines
have sugars that are necessary for entry into human
cells
Anthracyclines
Daunorubicin, idarubicin, doxorubicin, epirubicin, and valrubicin
Anthracyclines
are thought to form free radicals that can destroy DNA
Doxorubicin-iron
complexes
Epirubicin less __
than doxorubicin
cardiotoxic
affords cardioprotection caused by iron free radicals.
Dexrazoxane
for HIV cancer
Liposomal daunorubicin
Vincristine, vinblastine, vindesine, and vinorelbine are
plant alkaloids
inhibit microtubule
formation
plant alkaloids
inhibit depolymerization of microtubules
paclitaxel and docetaxel
Topotecan and irinotecan MOA
inhibit topoisomerase I
both contain sugars, inhibit topoisomerase II
etoposide and tenoposide
a weak estrogen receptor agonist
Tamoxifen
selective
estrogen receptor modulator (SERM)
Raloxifene
enzyme that converts testosterone into estrogen
P450 aromatase
by tri-imidazoles, anastozole and letrazole
P450 aromatase
bind iron in P450
enzymes
antifungal tri-imidazoles
exemestane and testolactone
Steroidal P450 aromatase inhibitors
irreversible steroidal P450 aromatase inhibitor
Exemestane
limits the usefulness of testolactone to three months use
Up-regulation of estrogen synthesis
disrupt estrogen
related hormone cycles
progestins
administered continuously to down-regulate
receptors responsible for releases of LH and FSH hormones
Leuprolide and goserelin
LHRH antagonist
Abarelix
Avoids testosterone surge and causes more
rapid medical castration
Abarelix
Effectiveness may decrease in time - failure detected by testosterone
level monitoring
Abarelix
can cause life-threatening allergic reactions
Abarelix
used in conjunction with LHRH therapies
Biclutamide and Flutamide
competes with dihydrotestosterone (the active form of testosterone) for binding to androgen
receptor
Bicalutamide
inhibits testosterone uptake into cells and binding to receptor
Flutamide
Estrogen receptor agonists
diethylstilbesterol and polyestradiol
an estrogen nitogen mustard
Estramustine
lead to low estrogen levels
estrogen receptor agonists
lowers prostate cancer risk but can be toxic
Selenium
is a potential vaccine to make antibodies that attack prostate cancer
Provenge
targets/binds prostatic acid phosphatase (PAP) on prostate cancer cells
Provenge
activate retinoic acid receptors which promote cell
differentiation or death
Tretinoin and Bexarotene
calcium receptor agonist
Cinacalcet
reduces parathyroid hormone secretion,
used to treat hypercalcemia in patients with parathyroid cancer
Cinacalcet
must dimerize in order to be active
Epitheleal Growth Factor Receptors