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CHMI 2227E Biochemistry I

CHMI 2227E Biochemistry I. Enzymes: Inhibition. Enzyme inhibition. VEGF-R. VEGF. Endothelial cell growth/migration. ZD6474. Endothelial cell. Enzyme inhibition Example 1 - VEGF Receptor inhibitors :. British Journal of Cancer (2005) 92(Suppl 1), S6 – S1. Vascular smooth muscle cell.

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CHMI 2227E Biochemistry I

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  1. CHMI 2227EBiochemistry I Enzymes: Inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  2. Enzyme inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  3. VEGF-R VEGF Endothelial cell growth/migration ZD6474 Endothelial cell Enzyme inhibitionExample 1 - VEGF Receptor inhibitors: CHMI 2227 - E.R. Gauthier, Ph.D. British Journal of Cancer (2005) 92(Suppl 1), S6 – S1

  4. Vascular smooth muscle cell Endothelial cell Acetylcholine GMP PDE Muscle relaxation Arginine Blood vessel Dilation Sildenafil Nitric Oxide Synthase (NOS) cGMP GTP Guanylate cyclase NO NO Enzyme inhibitionExample 2 – Sildenafil: Int. J. Impot. Res. (2004) 16, S11–S14 CHMI 2227 - E.R. Gauthier, Ph.D.

  5. Enzyme inhibitionExample 3 – Acetaminophen (tylenol): CHMI 2227 - E.R. Gauthier, Ph.D.

  6. P Trypsin inhibitor Reversible Enzyme inhibition1- Competitive inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  7. Reversible Enzyme inhibition1- Competitive inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  8. Reversible Enzyme inhibition2- Uncompetitive inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  9. Reversible Enzyme inhibition2- Uncompetitive inhibition • Vmaxapp= Vmax / (1 + [I]/Ki) • Kmapp= Km / (1 + [I]/Ki) CHMI 2227 - E.R. Gauthier, Ph.D.

  10. Reversible Enzyme inhibition3- Noncompetitive inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  11. Reversible Enzyme inhibition3- Noncompetitive inhibition • Vmaxapp= Vmax / (1 + [I]/Ki) CHMI 2227 - E.R. Gauthier, Ph.D.

  12. Irreversible enzyme inhibition CHMI 2227 - E.R. Gauthier, Ph.D.

  13. Irreversible enzyme inhibition1. Group-specific inhibitors CHMI 2227 - E.R. Gauthier, Ph.D.

  14. Irreversible enzyme inhibition2. Affinity labels CHMI 2227 - E.R. Gauthier, Ph.D.

  15. Irreversible enzyme inhibition3. Suicide inhibitors CHMI 2227 - E.R. Gauthier, Ph.D.

  16. Sugars Tetrapeptide pentaGly bridges Pen Structure of the bacterial cell wall Irreversible enzyme inhibition3. Suicide inhibitors - penicillin CHMI 2227 - E.R. Gauthier, Ph.D.

  17. Glycopeptide transpeptidase Glycopeptide transpeptidase pentaGly bridge Penicillin Tetrapeptide Glycopeptide transpeptidase Irreversible enzyme inhibition3. Suicide inhibitors - penicillin CHMI 2227 - E.R. Gauthier, Ph.D.

  18. Irreversible enzyme inhibition3. Suicide inhibitors - penicillin CHMI 2227 - E.R. Gauthier, Ph.D.

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