Term
| What are nuclear enzymes that reduce the supercoiled DNA torsional stress, allowing selected regions of DNA to become sufficiently untangled and relaxed to permit replication, recombination, repair and transcription to occur? |
|
Definition
|
|
Term
| What allows for relaxation of the DNA torsional strain, either by passage of the intact single-strand through the nick, or by free rotation of the DNA about the non-cleaved strand? |
|
Definition
| The cleavable complex that is formed when Topoisomerase I binds to the double stranded DNA through a reversible transesterification reaction that yields an intermediate complex in which the tyrosine of the enzyme is bound to the 3-Phosphate end of the DNA strand, creating a single strand DNA break |
|
|
Term
| What are the only topoisomerase I inhibitors used in cancer chemotherapy derivatives of? |
|
Definition
|
|
Term
| What two camptothecin derivatives are more water soluble and less toxic than the parent compound? |
|
Definition
|
|
Term
| Irinotecan is metabolized by cleavage of the R3 group to yield the active compound sometimes referred to as... |
|
Definition
|
|
Term
| Intestinal bacteria can enzymatically hydrolyze off the glucuronide to reform SN-38 in the GI tract, giving rise to... |
|
Definition
|
|
Term
| What is known to reduce levels of SN-38 by induction of cytochrome P450 and P-glycoprotein? |
|
Definition
|
|
Term
| What enzyme forms a covalent linkage to both strands of the DNA helix at the same time, making a transient double-strand break in the helix? |
|
Definition
|
|
Term
| What were the first two drugs of the anthracycline class discovered as antibiotics produced by Streptococcus peucetius? |
|
Definition
| doxorubicin and daunorubicin |
|
|
Term
| What are the drugs in the anthracycline class that are produced synthetically? |
|
Definition
Idarubicin
Valrubicin
Epirubicin |
|
|
Term
| The quinone-hydroquinone system is responsible for this color of the anthracyclines |
|
Definition
|
|
Term
| A liposomal form of doxorubicin is available for the treatment of... |
|
Definition
|
|
Term
| Use of the liposomal form of doxorubicin can give rise to... |
|
Definition
|
|
Term
| What enzyme causes the dismutation of superoxide and produces highly reactive hydroxyl radicals and hydrogen peroxide? |
|
Definition
|
|
Term
| What is a major side effect associated with anthracyclines? |
|
Definition
|
|
Term
| The chronic form of _______ is cumulative dose related in association with anthracyclines. |
|
Definition
|
|
Term
| What is the mortality rate of the chronic form of cardiomyopathy in association with anthracyclines? |
|
Definition
|
|
Term
| This iron chelator can be used to protect against cardiomyopathy associated with anthracyclines. |
|
Definition
|
|
Term
| This anthracenedione derivative has limited ability to produce quinone-type free radicals and causes less cardiotoxicity than does doxorubicin. |
|
Definition
|
|
Term
| Mitoxanthrone is approved for reducing neurologic disability in some forms of... |
|
Definition
|
|
Term
| This agent was extracted from the mandrake plant. |
|
Definition
|
|
Term
| What two derivatives of podophyllotoxin have their antitumor properties derive from their ability to complex with DNA and topoisomerase II, resulting in double strand breaks and cell death? |
|
Definition
|
|
Term
| The most important use of dactinomycin is in the treatment of _____ |
|
Definition
| rhabdomyosarcoma and Wilms' tumor |
|
|
Term
| What antibiotic intercalates into DNA between adjacent G-C base pairs of DNA and block transcription of DNA by RNA polymerase? |
|
Definition
|
|
Term
| Bleomycin is a mixture of what two water-soluble glycopeptide antibiotics? |
|
Definition
| bleomycin A2 and bleomycin B2 |
|
|
Term
| What drug is highly active in combination with other drugs in squamous cell carcinomas of the head and neck, esophagus, and genitourinary tract? |
|
Definition
|
|
Term
| What drug causes scission of DNA by interacting with O2 and Fe to generate free radicals that cut the deoxyribose backbone of the DNA chain? |
|
Definition
|
|
Term
| What is the most serious adverse reaction to bleomycin? |
|
Definition
|
|
Term
| What enzyme is bleomycin degraded by? |
|
Definition
|
|
Term
| Hydrolase, which degrades bleomycin, has low activity in what organs, causing toxicity in these organs? |
|
Definition
|
|
