Competitive Inhibition
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description
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 - PowerPoint PPT Presentation
Transcript of Competitive Inhibition
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Competitive Inhibition
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Competitive Inhibition
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Uncompetitive Inhibition
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Mixed Inhibition
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Inhibiting a Carboxypeptidase
• Carboxypeptidases bind peptides and cleave peptide bonds
• Design inhibitor that matches the active site
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Inhibiting ACE
• Complementary inhibitors
• Thiols are effective
• First generation motif may be tested
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Finding the Best Inhibitor• Synthesize and
test a number of compounds
• Find one with lowest Ki
• Captopril very effective, but side effects
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Second Generation Motif
• Make inhibitor that binds to more of enzyme
• Expand to a new subsite
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Modern Drug Design
Lisinopril (Merck) Hydroxyphosphinyloxy(Squibb)
Oral availability, metabolic stability, toxicity must be considered