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Tumor Cell Resistance
Pharmacology Exam 3
13
Pharmacology
Professional
04/01/2013

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Cards

Term
increased cellular capacity for DNA repair; cross resistance to other alkylating agents
Definition
mechloroethamine
Term
decreased active transport of drug into cells and altered form of FH2 reductase (minor); tumore cells generate an increased concentration of FH2 reductase through gene amplification (major)
Definition
methotrexate
Term
increased sythesis of thymidylate synthetase; altered affinity of TS for FdUMP; increased rate of catabolism of drug
Definition
5-FU
Term
depressed level of kinase required for activation leading to lack of phosphorylation and decreased inhibition of DNA synthesis; enhanced levels of deaminase that inactivates the drug
Definition
Cytarabine
Term
decreased drug activation by HGRPT; increases inactivation by alkaline phosphatase
Definition
6-MP and 6-TG
Term
reduced intracellular accumulation of drug due to increased efflux; amplification of the MDR1 gene/P170 GP (multidrug resistance MDR phenotype)
Definition
anthracyclines; daunorubacin, doxorubacin and mitoxantrone
Term
MDR
Definition
efflux pump with 12 binding domains, major clinical pproblem
Term
reduced intracellular accumulation (like P170 MDR gp); activation or enhancement of DNA repair mechanisms; increased glutathione transferase (GTS) activity
Definition
mitomycin
Term
high levels of drug hydrolase activity (lacking in skin and lungs); tumor cell mutation, altering the sequence that is sensitive to intercalation
Definition
bleomycin
Term
MDR phenotype
Definition
vincristing, vinblastin
Term
MDR phenotype
Definition
paclitaxel and docetaxel
Term
MDR phenotype
Definition
TPT (topotecan), CPT-11 (irinotecan)
Term
MDR phenotype
Definition
Etoposide or VP-16
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