Drugs Flashcards
AZT (azidothymidine)
- nucleoside analogue of thymidine
- anti-viral
- no free 3’ OH group = chain termination
- has high affinity for reverse transcriptase
- Treatment for HIV
Didanosine (ddl)
- nucleoside analogue of adenosine
- no free 3’ OH group = chain termination
- high affinity for reverse transcriptase
- Treatment for HIV
Acyclovir
- nucleoside analogue of guanosine
- has an open chains instead of a closed pentose sugar ring
- no free 3’ OH group
- viral thymidine kinase = 1st phosphorylation
- Treatment for herpes = only attacks infected cells and does not touch healthy cells because it can only be phosphorylated by viral thymidine kinase which is only in infected cells
Tenofovir
- nucleotide analogue of adenosine monophosphate
- open chain instead of pentose sugar ring
- no free 3’ OH group = chain termination
- treatment for HIV infections
Cytosine arabinoside (araC) aka cytarabine
- nucleoside analogue of cytosine - anti-cancer
- has 3’OH group, but there is a 2’ OH group too = steric hinderance!
- chain termination
- treatment for leukemia [myeloid + lymphoma]
Adenosine Arabinoside (araA) aka vidarabine
- nucleoside analogue of adenosine - anti-caner
- has 3’OH group, but there is a 2’ OH group too = steric hinderance!
- chain termination
- treatment for anti-neoplastic agent, relapsed childhood acute lymphoblastic leukemia and herpes simplex infections
Decitabine
- nucleoside analogue of cytidine - hypomethylation agent
- removes a methyl group
- prevent DNA methyltransferase enzymes from methylating cytosine - remember because DNA methylation is an important mechanism of gene regulation euk.
- important for transcriptional regulation
- use as a anti-methylator to counteract cancer cells
azacytidine
- nucleoside analogue of cytidine - hypomethylation agent
- removes a methyl group
- prevent DNA methyltransferase enzymes from methylating cytosine - remember because DNA methylation is an important mechanism of gene regulation euk.
- important for transcriptional regulation
- use as a anti-methylator to counteract cancer cells
Ciprofloxacin (Quinolone type)
- inhibits topoisomerase II (bacterial DNA gyrase)
- positive supercoils are not unwound
- treatment of respiratory and urinary tract infections and can also be used to treat anthrax
Camptothecin
- anti-cancer drug
- binds to and inhibits topoisomerase I = DNA breakage
- inhibits replication
Etoposide
- anti-cancer drug
- inhibits the activity of topoisomerase II (DNA gyrase) = DNA breakage
- inhibits replication
Actinomycin D (Dactinomycin)
- binds between G-C bases
- inhibits replication by prevent ssDNA and inhibiting RNA transcription
- anti-cancer drug, not normally used as an antibiotic
Rifampin
- Antibiotic
- from a strain of streptomycin
- inhibits transcription initiation by blocking the formation of the 1st phosphodiester bond
- RNA polymerase is not affected
- treatment for tuberculosis
Amanita Phalloides
-produces alpha amanitin which inhibits RNA polymerase II (mRNA)
Novobiocin
- inihibits topoisomerase II (DNA gyrase)
- positive supercoils are not unwound
What do Rotenone piericidine A (bacterial antibiotic) barbiturate amytal do?
Inhibit NADH dehydrogenase in Complex I
What do CO Azide Hydrogen Sulphide (H2S) Cyanide (CN-) do?
Inhibit cytochrome oxidase (Complex IV)
what does Antimycin A (antibiotic) do?
Inhibits cytochrome b of cytochrome reductase (Complex III)
what does Oligomycin (Streptomyces antibiotic) do?
Inhibits ATP synthase (Complex V)
what do ETC inhibitors do?
decrease ATP synthesis, decrease ETC and oxygen consumption
what does Atractyloside
Bongkrekic Acid
do?
Inhibits ADP/ATP transport; inhibits function of nucleotide translocase
what do DNP (dinitrophenol) ASA (aspirin) Thermogenin Ionophores do?
Destroy the protein gradient
what do Ionophores
• Gramicidin = channel formers
• Valinomycin = mobile carrier
do?
Make inner mitochondrial membrane permeable to compounds that can’t usually cross (small molecules now can get through)
what do uncouplers do?
decrease ATP synthesis, increase ETC, increase oxygen consumption
what do uncouplers and ionophores do?
allow for dissipation of the proton gradient
Streptomycin
Family of antibiotics with aminoglycoside structure
Prevents assembly of ribosome by binding to 30S subunit
Tetracycline
Family of antibiotics with four (tetra) ring (cyclic) structure
Blocks elongation by binding to 30S subunit and blocking the access of the aminoacyl-tRNA access to the A-site on the mRNA-ribosomal complex
Erythromycin (clindamycin)
Family of antibiotics and has macrolide structure
Binds to the 50S subunit of the complete 70S ribosome of bacteria and blocks ribosome translocation
Chloramphenicol
nhibits peptidyl transferase activity
May inhibit mitochondrial translation
Not broadly used because potential to develop decrease WBC
Important in some cases – some meningitis conditions
Cycloheximide
Inhibits peptidyl transferase activity May inhibit mitochondrial translation Toxic to eukaryotes Prokaryotes and mitochondria not affected Important experimental tool (cheap)
Puromycin
Analog of aminoacyl-tRNA
Toxic to both prokaryotes and eukaryotes translation
It’s a chain terminator in protein synthesis
Diphtheria toxin
C. diphtheria + bacterial virus
Causes diphtheria – lethal disease of respiratory tract
The A fragment of the toxin catalyzes the ADP-ribosylation of EF-2 = inhibiting translocation in eukaryotes
