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19 Cards in this Set

  • Front
  • Back
most commonly studied yeast strains (completely seq genome)
S. cerevisiae and S.pombe
3 problems in trying to target cancer cells:
1) lack of distinguishing properties-- many drugs are too non-specific to be helpful; 2) immune invisibility 3) development of resistance
3 main purposes of antimets as chemo drugs:
1) block synthesis of DNA precursors, 2) block DNA synthesis, 3) block replication
4 major mechanisms of action:
1) competitive inhibition of enzymes needed to synthesize DNA precursors 2) pseudo-feedback inhibitors of these pathways 3) inhibitors of DNA polymerase 4) intercalating agents
6 considerations in antimet efficacy:
1) cellular uptake 2) activation 3) specificity 4) toxicity 5) rate of degradation 6) development of resistance
sequinivir is a ______
HIV protease inhibitor
fuzeon is _____ that targets the protein ______
HIV fusion inhibitor, gp41
gleevec targets a constitutively active _____ that results in _______ signaling as a result of translocation and fusion of the _____ gene; it is used as a therapy for ____
kinase, GF-independent, bcr-abl; CML
influenza neuroamidase removes ____ cell-surface receptors
sialic acid
inhibitors of one-carbon of metabolism should block
purine synth and dTMPsynth
methotrexate is an analog of _____; it is a competitive inhibitor of __________, thus, it lowers intracellular ______ which reduces ________ and _______
folic acid; DHF reductase; 1-C derivatives; purine de novo synth and thymine synthase activity
6-MP is an inhibitor of ________; it is activated to _____ by ______; it works by _____ and ____; resistance develops if there is decreased ______ (less activation) or increased degradation via TPMT or ________ activity
de novo purine synth; activated to T-IMP by HGPRTase; feedback inhibition of PPRP amdiotransferase, inhibiting binding of IMP; HGPRTase, xanthine oxidase
______ is an inhibitor of DNA synthesis that is an analog of UMP/dUMP; it is a competitive inhibitor of _______ and is usually given in conjunction with ____, which repopulates the THF pool but also increases dFUMP inhibition
5-FU, thymidylate synthase, leucovorin,
mechanisms of resistance to 5-FU include: 1) increased ability of _______ to discrimiate btw dUMP and dFUMP; 2) overexpression of _____; 3) increased levels of dihydripyramidine dehydrogenase, which _________
thymidylate synthase; thymidylate synthase; degrades dFUMP
cytosine arabinoside is an inhibitor of ______; it is an analog of ____ and therefore a competitive inhibitor of ______
DNA synth; dCTP; DNA synth
Gemcitobire is a weak inhibitor of _______
DNA polymerase
HER2 is a member of the HER family of which also includes ______; in patients whose tumors show HER2 gene amp, ______, a __________, can be used to slow cell proliferation
RTKs, EGFR; Herceptin, a monoclonal antibody
_______ is an EGRF receptor antagonist; indications for use are in:
Tamoxifen; post-menopausal women with ER-positive cancer
To create conditional mutant mouse models, international initiatives have been coordinated to take advantage of ________ recombination.
Cre/LoxP