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Competitive Inhibition

Competitive Inhibition. Competitive Inhibition. Uncompetitive Inhibition. Mixed Inhibition. Inhibiting a Carboxypeptidase. Carboxypeptidases bind peptides and cleave peptide bonds Design inhibitor that matches the active site. Inhibiting ACE. Complementary inhibitors Thiols are effective

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Competitive Inhibition

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  1. Competitive Inhibition

  2. Competitive Inhibition

  3. Uncompetitive Inhibition

  4. Mixed Inhibition

  5. Inhibiting a Carboxypeptidase • Carboxypeptidases bind peptides and cleave peptide bonds • Design inhibitor that matches the active site

  6. Inhibiting ACE • Complementary inhibitors • Thiols are effective • First generation motif may be tested

  7. Finding the Best Inhibitor • Synthesize and test a number of compounds • Find one with lowest Ki • Captopril very effective, but side effects

  8. Second Generation Motif • Make inhibitor that binds to more of enzyme • Expand to a new subsite

  9. Modern Drug Design Lisinopril (Merck) Hydroxyphosphinyloxy (Squibb) Oral availability, metabolic stability, toxicity must be considered

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