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Module 1 Biochem > Drugs > Flashcards

Drugs Flashcards

1
Q

azidothymidine (AZT)

A
  • Nucleoside analogue of deoxythymidine
  • No free 3’OH
  • Host kinase phosphorylates it to activate it
  • Incorporated into DNA chain via viral reverse transcriptase
  • Termination occurs
  • Given to HIV patients
  • Reduces risk of mother to baby transmission of HIV
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2
Q

didanosine

A
  • Nucleoside analogue of deoxyadenosine
  • No free 3’OH
  • Viral reverse transcriptase incorporates it
  • Termination of viral replication
  • Has high affinity for reverse transcriptase but low affinity for DNA pol
  • Given to HIV patients
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3
Q

acyclovir

A
  • Nucleoside analogue of deoxyguanosine
  • No free 3’OH
  • Converted to monophosphate acyclovir initially via viral kinase
  • Only activated in infected cells
  • Phosphorylation later via host kinase
  • Stop DNA elongation
  • Treats Herpes and varicella zoster
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4
Q

tenofovir

A
  • nucleotide analogue of deoxyadenosine monophosphate
  • No free 3’OH
  • Competes with deoxyadenosine
  • Initially activated by host kinase
  • Lack of 3’OH terminates replication
  • Treats HIV
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5
Q

cytarabine/vidarabine

A
  • Sugar analogue
  • Has 3’OH and 2’OH
  • 3’ end accepts elongation
  • But 2’OH inhibits addition of next dNTP due to steric hindrance, which stops chain elongation
  • Antineoplastic (anti tumor) agent
  • Herpes simplex
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6
Q

decitabine

A
  • Nucleoside analogue of deoxycytidine
  • Hypomethylation agent
  • Once incorporated into DNA/RNA – does hypomethylation
  • Blocks methylation –> keeps acetyl groupss
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7
Q

ciprofloxacin and nalidixic acid

A
  • Antibiotic fluoroquinolone
  • Inhibits bacterial DNA gyrase (type II topoisomerase) which is absent in euks
  • Leads to positive supercoil buildup, and ultimately chain termination
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8
Q

novobiocin

A
  • antibiotic, courmarin family
  • Inhibits bacterial DNA gyrase (type II topoisomerase), which is absent in euks
  • Leads to positive coil buildup and ultimately, chain termination
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9
Q

camptothecin

A
  • Anti-cancer
  • Inhibits topoisomerase I activity, which leads to DNA breakage
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10
Q

etoposide

A
  • Anti-cancer
  • Inhibits the activity of topoisomerase II actvity
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11
Q

actinomycin D

A
  • Anti-cancer
  • Planar phnoxazone ring intercalates adjacent G-C bases
  • Prevents formation of regions of ss DNA
  • Prevents RNA transcription as it prevents strand separation
  • Inhibitor of replication and transcription
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12
Q

rifamycin (rifampin)

A
  • Antibiotic that treats tuberculosis
  • Blocks formation of 1st phosphodiester bond by binding to prok RNA pol –> conformation change in RNA pol –> inhibits initiation of transcription
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13
Q

diptheria toxin

A
  • Inactivation of EF-2 by ADP ribosylation, which prevents translocation
  • Affects protein synthesis and translation
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14
Q

streptomycin

A
  • prevents assembly of ribosome (binds to 30S subunit)
  • treats bacterial infections
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15
Q

tetracyclin

A
  • Interacts with 30S subunit of complete 70S ribosome
    • blocks elongation by blocking aminoacyl-tRNA access to A site
  • treats bacterial infection
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16
Q

erythromycin (macrolide)

A
  • binds to 50S subunit of the complete 70S structure
    • blocks ribosome translocation
  • treats bacterial infection
17
Q

chloramphenicol

A
  • inhibits peptidyl transferase activity in prokes
  • however, at high doses, it can inhibit mitochondrial translation
18
Q

cycloheximide

A
  • Inhibits euk peptidyl transferase activity
    • OPPOSITE of chloramphenicol
19
Q

puromycin

A
  • causes premature termination of translation in both prokes and euks by preventing elongation
  • structural analog to part of aminoacyl tRNA
20
Q

alpha-aminitin toxin

A
  • found in Death Cap mushroom
  • Inhibits RNA pol II in euks and prevents mRNA formation
  • Treatment
    • GI decontamination
    • penicillin
    • liver transplant
21
Q

colchicine

A
  • prevents polymerization by binding to unpolymerized tubulin molecules
  • if given to dividing cells, mitotic spindle breaks down and leads to programmed cell death
  • anti-cancer
  • Used in treatment of gout
    • ​prevents migration of white blood cells to joints
22
Q

taxol

A
  • stabilizes and prevents microtubule disassembly
    • preferentially binds tubulin within assembled microtubules
  • anti-cancer
23
Q

cytochalasins

A
  • similar to colchicine in microtubules
  • prevents actin polymerization
    • inhibits cell movement, division and induces apoptosis
  • fungal product
24
Q

phalloidin

A
  • similar to taxol in microtubules
  • prevents disassembly of actin polymers
    • promotes excessive polymerization and inhibits depolymerization
  • inhibits cell movement
  • toxin from Death Cap mushroom
25
Q

sulfamides/sulfa drugs

A
  • inhibit the folic acid synthesis from PABA to folic acid
  • inhibit bacterial folate synthesis
26
Q

trimethoprim

A
  • inhibits bacterial dihydrofolate reductase
    • prevents the production of tetrahydrofolate (THF)
27
Q

methotrexate

A
  • inhibits the function of dihydrofolate reductase
    • reduces the amount of tetrahydrofolate available for purine synthesis and slows down DNA replication in euks
  • Anti-cancer
28
Q

hydroxyurea

A
  • inhibits ribonucleotide reductase
    • prevents ribonucleoside diphosphate from turning into deoxyribonucleoside diphosphate
  • Anti-cancer
29
Q

allopurinol

A
  • structural analog of hypoxanthine
    • non-competitive irreversible inhibitor
  • inhibits xanthine oxidase
    • decreases the formation of uric acid
    • used in overproducers
30
Q

febuxostat

A
  • xanthine oxidase inhibitor
    • febuXOSTat: xanthine oxidase stops
31
Q

5 fluorouracil

A
  • 5 fluorouracil converts to 5 fluoro dUMP and inhibits thymidylase synthase
    • binds to it irreversibly and inactivates it (suicide inhibitor)
  • anti-cancer
32
Q

mycophenolic acid

A
  • inhibits formation of GTP from IMP
    • reversible uncompetitive inhibitor
    • blocks enzyme IMP dehydrogenase
    • deprives rapidly proliferating B and T cells of key components of nucleic acids
    • used to prevent graft rejections
33
Q

nitroprusside/nitroglycerin

A
  • anti-hypertensive
  • metabolized by the body to produce NO
34
Q

cholera toxin

A
  • an enzyme that ADP-ribosylates Gαs resulting in continuously active Gαs
    • destroys the intrinsic GTPase activity, which means Gαs is always on
      • constantly creates cAMP, which leads to dysentery
35
Q

pertussis toxin

A
  • an enzyme that ADP-ribosylates Gαi to make it continuously inactive
    • cAMP increased in respiratory-tract cells
    • respiratory distress and whooping cough
36
Q

di-isopropyl fluorophosphate (DFP)

A
  • Irreversible inhibitor of acetylcholinesterase
    • acetylcholinesterase normally cleaves the neurotransmitter acetylcholine in the postsynaptic neuromuscular junction
  • at the active site: serine normally forms a covalent bond with the acetyl group during catalysis. DFP blocks this reaction
37
Q

aspirin

A
  • Aspiring irreversibly inhibits COX in both platelets and endothelial cells
    • endothelial cells degraded the modified enzyme and synthesize new COX that is fully active
      • endothelial cells produce prostacyclin, which prevents blood clotting
    • blood platelets are not able to synthesize new COX and less thromboxane is finally released
      • thromboxane stimulates blood clotting
  • Aspirin is acetyl-salicylic acid and it acetylates a serine in the channel of the active site of COX
38
Q

statin

A
  • competitive reversible inhibitor
  • inhibits HMG CoA reductase, the regulated enzyme of cholesterol synthesis.

Module 1 Biochem (12 decks)

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