Wimmer Therapeutic applications of enz. inhib.
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What does penicillin target?
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Cell wall peptidoglycan biosynthesis.
Transpeptidase.
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What are some treatments for organophosphate poisoning?
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Atropine: ACh antagonist buys time to make new AChE
Pralidoxime: chemically reverses ser modification
- Tell me about myasthenia gravis.
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Decrease amounts of ACh receptors. Use pyridostigmine bromide as an AChe inhibitor; increasing levels of ACh.
(Reversible)
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What do organophosphates do?
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Fom the acyl-E intermediate, but don't leave. (Suicide inhibitor)
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How does transpeptidase work?
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Active site ser attacks D-ala-D-ala peptide bond; forms acyl-enz. intermediate.
Crosslink: gly of pentaglycine bridge accepts acyl group
- How does penicillin work?
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Beta-lactam ring.
(Also a thiazolidine right)
Substrate analog; forms acyl-enz. intermediate.
Penicilloyle-enzyme is inactive, blocking crosslinking
Osmotic lysis
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Penicillin resistance and ways to fight it.
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Beta-lactamase cleaves beta-lactam.
Augmentin: amoxicillin and clavulanic acid.
Clavulonic acid: suicide inactivator of
beta-lactamase