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Antimicrobials Targets to Inhibit (Protein Synthesis (streptomycin…
Antimicrobials Targets to Inhibit
Protein Synthesis
Prokar: 70S ribosome with 50S and 30S ribosome
drugs do affect humans bc mitochondria has 70S
streptomycin (aminoglycosides)
bind to 30S, disrupt EPA site and codons/reading frame
tetracycline
Binds to tRNA, A-site
chloramphenicol
prevent peptide bond formation between AA's
erythromycin (Macrolides)
halt ribosome movement
antisense RNA
strand complementary mRNA blocks ribosomal subunit to that mRNA
Cell wall synthesis
Beta-Lactams
competitively inhibit NAM-NAM cross-linking
Bacterial Resistance: beta lactamase
Effective only against growing, reproducing bacterial cells in log phase, NO effect against cell wall that is already there
Cytoplasmic Membranes
amphotericin B - antifungal
target unique lipid: ergosterol in fungal membranes
ergosterol is similar to cholesterol, so humans are a bit susceptible, but ergosterol binds more strongly to amphotericin B
forms pore in membrane that destroys the selective permeability of a cell membrane
Metabolic pathways
target enzymes of pathogen
sulfonamides/sulfa drugs
sulfanilamide
analog to PABA used in nucleotide synthesis for DNA, RNA synthesis
acts as metabolic antagonist, competitive inhibitor to PABA
prevents PABA's conversion to dihydrofolic acid
trimethoprim
prevents conversion of dihydrofolic acid to tetrahydrofolic acid (THF)
Attachment
Example: Influenza
enveloped, 2 proteins embedded
(H) hemagglutinin
has affinity to the sialic acid residues on host cell membrane
(N) Neuraminidase
severs bond between H and sialic acid to "free" new virus from host cell
Tamiflu, Relenza
Prevent release of new viruses from host cell by competitively inhibiting neuraminidase (N)