Term
| siRNA True 1. They have a length of approximately 21-23 nucleotides 2. They are double stranded 3. they inhibit gene expression by degrading homologous mRNA |
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Definition
| si RNA False: 1. they inhibit replication by annealing to homologous DNA sequences 2. they work by a posttranslational gene splicing mechanism 3. they cleave transcription factors, thereby inhibiting gene expression |
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Term
| Which statements about chemical (compositional) and regulatory differences between natural drugs and herbal remedies (botanical dietary supplements) are true? |
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Definition
● Herbal remedies are mixture compounds
● Herbal remidies don’t require FDA approval
● Natural product drugs are usually given single agents |
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Term
| Give reasons for potential problems associated with toxicity and/or lack of activity |
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Definition
● Contamination with pesticides/herbicides/heavy metals
● Use of incorrect part of plant
● Active component not present or has inconsistent amounts
● Active compound produced by a microorganism
● Interactions with other botanicals or medications (not rigorously tested) |
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Term
| Which of the following are NOT marine natural products |
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Definition
● TAXOL
● ERYTROMYCIN
● CYCLOSPORIN A |
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Term
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Definition
● Taxol is diterpenederived
● An isoprene unit consists of five carbons
● Cocaine is an alkaloid
● Peptides and polypeptides are commonly synthesized by bacteria |
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Term
| Which two statements are true about the drugs GLEEVEC, TYKERB, and NEXAVAR |
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Definition
-They inhibit kinases
● They inhibit intracellular signaling to transcription factors |
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Term
| Associate the herbal remedies with the claims/potential applications |
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Definition
Antidepressant=St. john’s wort
● Antiseptic, antiviral, immunostimulant=Echinacea
● Antiinflammatory, antiasthmatic, treatment for dementia=Ginko
● Stamina, stress resistance, healing, against age associated degeneration=Ginsing |
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Term
| Describe the mech of action (MOA) of histone deacetylase (HDAC) inhibitors and explain why they may be useful for anticancer therapy. |
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Definition
By preventing the deacetylation of histone, HDAC inhibitors r educe electrostatic interactions between negatively charged DNA and positively charged lysine residues of histones, thereby loosening the chromatin and activate gene expression
● Reactivation of tumor suppressor genes or regulators/inhibitors of the cell cycle may have anticancer effects |
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Term
| Describe the MOA of indirect antioxidants via transcription factor Nrf2 and give one example of a phytochemical/vegetable with that activity. |
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Definition
| They induce the nuclear translocation of Nrf2. Nrf2 then binds a DNA sequence in the promoter region of the genes encoding antioxidant and detoxification enzymes, leading to their gene expression and subsequently increased antioxidant status in the cell. |
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Term
Assume you find a sponge during a collection trip with the Luesch group in the
Florida Keys and back at UF you isolate an active compound that structurally appears to be a peptidepolyketide hybrid. Six months later you recollect the sponge from the same dive site, however, you don’t find the same compound again. Give 2 reasons why. |
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Definition
● Seasonal variation in metabolite production
● Compound may be produced by a symbiotic organism/bacterium that wasn’t present six months ago |
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Term
| . Assume you have discovered an anticancer compound w/ toxic SEs on normal cells. Provide strategies to increase the therapeutic window of the agent. |
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Definition
● Structural modification may lead to improved selectivity
● Conjugation to an antibody could assure preferential delivery to the tumor target site |
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Term
| Give reasons why protease inhibitors may be useful for cancer therapy |
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Definition
| ● Protease inhibitors stabilize certain proteins by preventing or retarding their degradation. Therefor they may be able to stabilize tumor suppressors and/or endogenous cell cycle inhibitors and/or cytoplasmic inhibitors of cancer associated transcription factors |
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