General Chemistry II Course
Competencies
Lsn 15: Nonsteroidal Anti-Inflammatory Drug (NSAID's)
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Understand the inflammation mechanism of action initiated by arachidonic
acid (phospholipid release of arachidonic acid, generation of prostaglandins
and thromboxanes through cyclooxygenase pathway, generation of leukotrienes
through lipoxygenase mechanism)
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Understand the mechanism of action of cyclooxygenase (COX) inhibitors
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Identify key structural features of NSAIDs and understand of specific important
interactions with COX enzymes
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Understand the specific interaction between the NSAID carboxylic group
and the COX Arg-120 side chain; describe and effectively explain the effect
upon Km values that occur when neutral glutamine is substituted
for Arg-120
Understand and clearly discuss aspirin's unique mechanism of action
for irreversible COX inhibition
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COX-2 Inhibitors
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Understand key differences between COX-1 and COX-2 enzymes, their physiological
roles, and their respective inhibitors
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Clearly describe the rationale for the development of COX-2 inhibitors
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Explain the structure differences between nonspecific COX inhibitors and
COX-2 specific inhibitors; relate these differences to active site geometries
of thee two enzymes
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Use COX-1 and COX-2 IC50 values for various substances to evaluate their
respective potential for therapeutic development