lecture 40: eicosanoids Flashcards
what is the fatty-acid needed for eicosanoid synthesis
arachidonic acid
what 4 things can arachidonic acid give rise to
leukotrienes, prostaglandin H2, prostacyclin, thromboxane
what does prostaglandin H2 synthase do
acts on arachidonic acid to form PGG2, and then acts on PGG2 to form PGH2
what enzyme cleaves arachidonic acid from phospholipids
phospholipase A2
what is the mechanism of the anti-inflammatory process of NSAIDs
they bind to the tunnel in the ER where arachidonic acid has to travel through to reach the active site; block enterancec of arachidonic acid
type of inhibitor that Aspirin is
non-selective, suicide inhibitor
type of inhibitor that ibuprofen and naproxen are
non-selective, competitive inhibitors
non-selective NSAIDs block what
COX-1 and COX-2
what does prolonged usage of non-selective NSAIDs cause
GI ulcers or bleeding due to longer inhibition of COX-1
selective NSAIDs block what
COX-2 only
celecoxib and rofecoxib are drugs that block what
COX-2; selective inhibitor
what does prolonged usage of selective NSAIDs cause
increased risks of heart attacks
why is prolonged usage of selective NSAIDs bad mechanistically
prostacyclin is regulated by COX-2 for the regulation of blood vessels and clotting. when it is un-regulated it can cause clots by thromboxane accumulation
