drugs Flashcards
fluoroquinolone target
termination of bacterial DNA replication
fluoroquinolone MOA
inhibits gyrase and topo IV so it inhibits both gram pos/neg bacteria
topoisomerase poisons target
Eukaryote DNA
replication
topoisomerase poisons MOA
Trap topo:DNA
complex -> cause single
and double-strand DNA breaks
topo trap
topoisomerase uses
cancer therapy
Alkylating agents target
Modification of DNA
Alkylating agents MOA
Interstrand cross-link to DNA
Crosslinking agents target
Modification of DNA
Crosslinking agents MOA
Intrastrand cross-link DNA
Rifampicin target
prokaryotic RNAP
Rifampicin MOA
binds to beta subunit>prevent movement of sigma factor>RNAP cannot interact w/promoter>prevent transcription at early stage
prevent interaction with beta sigma fam
alpha-amantitin target
eukaryotic RNAP 2
alpha-amantitin MOA
inhibit RNAP>inhibit elongation phase of transcription
Rifampicin uses
tuberculosis
Rifampicin resistance
2 ways:
1) bacteria acquires mutations at particular positions around the binding site
2) expressing Arr: ADP-ribosylates Rifampicin
RNAi therapy target
deleterious genes (mRNA)
RNAi therapy MOA
forms RISC, binds miRNA and mediates formation of duplex btwn guide strand and mRNA, prevents translation by stim degradation of polyA tail
RNAi therapy uses
treatment of hereditary transthyretin-mediated amyloidosis
Tetracycline MOA
delivery of activated tRNA to A site by elongation factor EF-Tu inhibited
cycling=delivery
streptomycin MOA
inhibits GTP-powered proofreading by EF-Tu
“streps” away ability to read