Shared Flashcard Set

Details

Part 7: Targeted Molecular Therapies
N/A
27
Pharmacology
Graduate
01/06/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Which two drugs are cytosine analogs that inhibit DNA methylation at cytosine residues?
Definition
Azacytidine (Vidaza)
Decitabine (Dacogen)
Term
Azacytidine and decitabine are approved for the treatment of ___________________
Definition
Myelodysplastic syndrome (MDS)
Term
Both azacytidine and decitabine are converted to its corresponding 5'-triphosphate which is then incorporated into DNA where it blocks the action of DNA _______________
Definition
Methyltransferase
Term
_______________ are organized into an octamer known as a _______________ around which DNA is wound
Definition
Histones
Nucleosome
Term
Which enzyme causes acetylation of these L-amino groups reducing histone basicity, therefore exposing portions of the DNA to transcription factors which in turn leads to gene expression.
Definition
Histone acetyltransferase (HAT)
Term
Which class of enzymes remove the acetyl groups from the histone L-N-acetylated lysines?
Definition
Histone deacetylases (HDAC)
Term
________________ is a histone deacetylase inhibitor (HDAC inhibitor)
Definition
Vorinostat (SAHA)
Term
What does EGFR stand for?
Definition
Epidermal Growth Factor Receptor
Term
What are the two major members of the EGFR family of proteins?
Definition
ErbB1 (EGF-R, HER1)
ErbB2 (HER2/neu)
Term
Which receptor is overexpressed in about 30% of breast cancers and because of this increased expression of the gene it correlates with poor prognosis.
Definition
HER2/neu receptor
Term
The HER2/neu receptor alone is the target of this monoclonal anitbody
Definition
Trastuzumab (Herceptin)
Term
Two antineoplastic monoclonal anitbodies both target the ErbB1 receptor
Definition
Cetuximab (Erbitux)
Panitumumab (Vectibix)
Term
Which drug inhibits the intracellular phosphorylation of the ErbB1 receptor which is overexpressed in certain lung cancers?
Definition
Gefitinib (Iressa)
Term
This drug is an inhibitor of HER1 tyrosine kinase, which is associated with the epidermal growth factor receptor
Definition
Erlotinib (Tarceva)
Term
This drug is a dual RTK inhibitor that inhibits both ErbB1 and HER2/neu
Definition
Lapatinib (Tykerb)
Term
This drug is used for the treatment of advanced renal cell carcinoma
Definition
Sofafenib
Term
This drug is an RTK inhibitor that is approved for the treatment of gastrointestinal stromal tumor (GIST) and renal cell carcinoma
Definition
Sunitinib
Term
The VEFG receptor is another RTK. What does VEFG stand for?
Definition
Vascular Endothelial Growth Factor
Term
This drug targets all 3 isoforms of the VEFG receptor and is used in the treatment of renal cell carcinoma
Definition
Pazopanib
Term
This drug which targets VEGF is approved for use with 5-FU in advanced colorectal cancer and with interferon-alpha in renal cell carincoma
Definition
Bevacizumab (Avastin)
Term
The chromosome translocation responsible for chronic myelogenous leukemia occurs because of an abnormal chromosome known as the ____________ chromosome
Definition
Philadelphia
Term
The philadelphia chromosome has the N terminus of the Bcr protein joined to the C terminus of the Abl protein tyrosine kinase (PTK) and as a result the Abl kinase domain becomes _______________________
Definition
Inappropriately (constitutively) active
Term
This drug was the first FDA approved drug targeted to a specific molecular defect in cancer and has been used orally in the treatment of chornic myelogenous leukemia
Definition
Imatinib (Gleevec)
Term
What does mTOR stand for?
Definition
Mammalian Target of Rapamycin
Term
What type of kinase is mTOR?
Definition
Serine/threonine protein kinase
Term
Which drug is able to inhibit mTOR through association with its intracellular receptor?
Definition
Sirolimus (Rapamycin)
Term
This mTOR inhibitor is approved for the treatment of advanced renal cell carcinoma
Definition
Temsirolimus
Supporting users have an ad free experience!