competitive inhibition
Post on 23-Feb-2016
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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
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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
• First generation motif may be tested
Finding the Best Inhibitor• Synthesize and
test a number of compounds
• Find one with lowest Ki
• Captopril very effective, but side effects
Second Generation Motif
• Make inhibitor that binds to more of enzyme
• Expand to a new subsite
Modern Drug Design
Lisinopril (Merck) Hydroxyphosphinyloxy(Squibb)
Oral availability, metabolic stability, toxicity must be considered
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