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Competitive Inhibition

Competitive Inhibition. C-OO - C-H C-H C-OO -. C-OO - H-C-H H-C-H C-OO -. C-OO - H-C-H H-C-H H-C-H C-OO -. C-OO - H-C-H C-OO -. C-OO - C-OO -. Substrate. Product. Competitive Inhibitor. Succinate. Glutarate. Malonate. Oxalate. Succinate Dehydrogenase.

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Competitive Inhibition

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  1. Competitive Inhibition C-OO- C-H C-H C-OO- C-OO- H-C-H H-C-H C-OO- C-OO- H-C-H H-C-H H-C-H C-OO- C-OO- H-C-H C-OO- C-OO- C-OO- Substrate Product Competitive Inhibitor Succinate Glutarate Malonate Oxalate Succinate Dehydrogenase Adapted from Kleinsmith & Kish (1995) Principles of Cell and Molecular Biology (2e) p.49

  2. Sulfa Drug Is Competitive Inhibitor -COOH H2N- -SONH2 H2N- Domagk (1939) Para-aminobenzoic acid (PABA) Bacteria needs PABA for the biosynthesis of folic acid Folic acid Tetrahydro- folic acid Precursor Sulfa drugs has similar structure with PABA, and inhibit bacteria growth. Sulfanilamide Sulfa drug (anti-inflammation) Adapted from Bohinski (1987) Modern Concepts in Biochemistry (5e) p.197

  3. Enzyme Inhibitors Are Extensively Used subunit 1 subunit 2 Asp Asp domain 1 domain 2 Asp Asp ●Sulfa drug (anti-inflammation) Pseudo substrate competitive inhibitor ●Proteaseinhibitor Alzheimer's disease Plaques in brain contains protein inhibitor ●HIV protease is critical to life cycle of HIV HIV protease(homodimer): ↑inhibitor is used to treat AIDS Symmetry →Human aspartyl protease: (monodimer) Not symmetry Juang RH (2004) BCbasics

  4. HIV protease vs Aspartyl protease subunit 2 subunit 1 Asp Asp domain 1 domain 2 Asp Asp HIV Proteaseinhibitoris used in treating AIDS ↓HIV protease (homodimer) Symmetric dimer Asymmetric monomer ↑Aspartyl protease (monomer) Juang RH (2004) BCbasics

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