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19 Cards in this Set
- Front
- Back
most commonly studied yeast strains (completely seq genome)
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S. cerevisiae and S.pombe
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3 problems in trying to target cancer cells:
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1) lack of distinguishing properties-- many drugs are too non-specific to be helpful; 2) immune invisibility 3) development of resistance
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3 main purposes of antimets as chemo drugs:
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1) block synthesis of DNA precursors, 2) block DNA synthesis, 3) block replication
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4 major mechanisms of action:
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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
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6 considerations in antimet efficacy:
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1) cellular uptake 2) activation 3) specificity 4) toxicity 5) rate of degradation 6) development of resistance
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sequinivir is a ______
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HIV protease inhibitor
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fuzeon is _____ that targets the protein ______
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HIV fusion inhibitor, gp41
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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 ____
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kinase, GF-independent, bcr-abl; CML
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influenza neuroamidase removes ____ cell-surface receptors
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sialic acid
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inhibitors of one-carbon of metabolism should block
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purine synth and dTMPsynth
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methotrexate is an analog of _____; it is a competitive inhibitor of __________, thus, it lowers intracellular ______ which reduces ________ and _______
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folic acid; DHF reductase; 1-C derivatives; purine de novo synth and thymine synthase activity
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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
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de novo purine synth; activated to T-IMP by HGPRTase; feedback inhibition of PPRP amdiotransferase, inhibiting binding of IMP; HGPRTase, xanthine oxidase
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______ 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
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5-FU, thymidylate synthase, leucovorin,
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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 _________
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thymidylate synthase; thymidylate synthase; degrades dFUMP
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cytosine arabinoside is an inhibitor of ______; it is an analog of ____ and therefore a competitive inhibitor of ______
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DNA synth; dCTP; DNA synth
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Gemcitobire is a weak inhibitor of _______
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DNA polymerase
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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
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RTKs, EGFR; Herceptin, a monoclonal antibody
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_______ is an EGRF receptor antagonist; indications for use are in:
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Tamoxifen; post-menopausal women with ER-positive cancer
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To create conditional mutant mouse models, international initiatives have been coordinated to take advantage of ________ recombination.
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Cre/LoxP
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