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36 Cards in this Set
- Front
- Back
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What is an inhibitor of the CML BCR-ABL tyrosine kinase?
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Gleevec
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What was previously called STI-571 (signal transduction inhibitor 571)?
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Gleevec
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Gleevec was designed to specifically inhibit the ___________.
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ABL tyrosine kinase
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Gleevec was found to inhibit the __________ activated by the ___________ in CML.
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BCR-ABL tyrosine kinase; chromosomal translocation
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Gleevec is effective in the trtmt of what?
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CML
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What induces apoptosis in bcr-abl active cells?
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Gleevec
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Gleevec inhibits the ______ tyrosine kinase and the _____ tyrosine kinase.
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PDGF; c-Kit
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RAF is a ___________ kinase.
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serine/threonine
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What drug is approved for the treatment of renal carcinoma?
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Nexavar
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What is an example of a "multikinase" inhibitor?
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Nexavar
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Nexavar is a kinase inhibitor that inhibits the ________ signal transduction pathway which has a role in promoting cell proliferation.
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RAF/MEK/ERK
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Nexavar inhibits the receptor tyrosine kinases ________ and ________ which have roles in promoting tumor angiogenesis which is necessary for tumor growth.
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PDGFR; VEGFR
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What are growth factor receptors?
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proteins that play a major role in regulating cell division (many are tyrosine kinases regulated by ligand binding to extracellular domains)
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PLC degrades phosphatidylinositol biphosphate (PIP2) to what?
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Diacylglycerol and inositol triphosphate
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What are examples of members of the EGF receptor tyrosine kinases?
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erbB oncogene and HER-2/neu proto-oncogene
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The erbB oncogene was first found in what?
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avian erythroblastosis virus
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The HER-2/neu proto-oncogene found amplified in what kind of tumors and in what percentage?
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30% of human breast tumors
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__________ is a monoclonal antibody which binds the ligand binding domain of HER-2 and slows growth of HER-2 positive tumors.
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Herceptin
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In the erbB protein structure, what happens to the ligand binding domain and the kinase?
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the ligand binding domain is deleted leaving the kinase in the active structure
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What happens when the growth factor (EGF) binds to the extracellular domain of its receptor?
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Kinase activation
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Growth factors ____ and _____ bind to EGF receptor and activate the EGFR pathway which is involved in what?
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EGF; TGF-α; involved in tumor cell growth, repair, angiogenesis, and metastasis
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What is the name of the monoclonal antibody that can inhibit the EGF receptor?
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Erbitux
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Erbitux binds to _____ and blocks the ability of growth factors to signal the tumor cell to divide.
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EGFR
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What can 90% of all cancer deaths possibly be attributed to?
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use of tobacco and dietary factors
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the "tar" of tobacco contains numerous _______ like benzpyrene that are converted in the body into what?
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polycyclic aromatic hydrocarbons (PAHs); potent alkylating agents for DNA
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Avastin specifically targets and binds to what thus inhibiting receptor activation and cell growth?
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The VEGF growth factor
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VEGF proteins bind to what?
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vascular Endothelial Growth Factor Receptor (VEGFR) also known as KDR
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When VEGF binds to VEGFR what happens?
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Activates a signal to the cell to initiate new blood vessel formation (angiogenesis)
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What monoclonal antibody binds to the VEGF (KDR) receptor and blocks circulating VEGF proteins from activating the receptor and send the signal to initiate angiogenesis?
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IMC-1C11
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Alkylating agents usually cause point mutations to occur in DNA resulting in what?
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codon base changes and amino acids substitutions
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In the ras G-protein proto-oncogene, changes to the oncogene form take place in what 2 codons? Some changes are ____ and some are _____.
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12 and 61; transitions; transversions
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What 2 steps are involved with rodent models for chemical carcinogenesis?
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1) initiation by introducing DNA mutations
2) promotion by a cell proliferating agent |
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_______ are important for understanding how events outside of genetics contribute to cancer formation.
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Tumor promoters
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Trtmt with polycyclic aromatic hydrocarbon carcinogens like _________ or _________ leads to DNA mutationsvia nucleotide base alkylations.
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Dimethylbenzanthracene (DMBA); bezpyrene (BP)
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Neoplasm development requires further trtmt with a cell proliferating agent (promoters) like _______ or _______.
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Diaclyglycerol (DAG); tetradeanoyl-phorbol acetate (TPA)
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Tumors will develop even if promotor trtmt is delayed for up to how long after the carcinogen trtmt?
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Up to a year
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