• Introduction
• 3 min
  1. Editor's foreword

  • Prof. Ann Daly
• 47 min
  2. Introduction to drug metabolism enzymes

  • Dr. Dennis Smith
• General factors affecting drug metabolism
• 30 min
  3. General factors affecting drug metabolism: effect of physiological factors and disease 1

  • Prof. Edward T. Morgan
• 24 min
  4. General factors affecting drug metabolism: effect of physiological factors and disease 2

  • Prof. Edward T. Morgan
• 39 min
  5. Drug metabolism in liver disease

  • Dr. Nathalie Zgheib
  • Prof. Robert Branch
• 37 min
  6. Laboratory methods for the in vitro study of drug metabolism

  • Dr. Ritu Singh
• 50 min
  7. Prediction of pathways of drug metabolism

  • Dr. Maurice Dickins
• Phase I metabolizing enzymes: cytochrome P450s
• 45 min
  8. Cytochrome P450 1 family: the roles of 1A1, 1A2 and 1B1 in drug metabolism

  • Prof. F. Peter Guengerich
• 42 min
  9. CYP2 family

  • Prof. Ann Daly
• 52 min
  10. Why study the cytochrome P4503A (CYP3A) family?

  • Dr. Erin Schuetz
• 54 min
  11. Pharmacogenomics: an update

  • Prof. Magnus Ingelman-Sundberg
• Phase I metabolizing enzymes: non-cytochrome P450s
• 45 min
  12. Non-P450 oxidative metabolism: characteristics and drug substrates

  • Dr. Christine Beedham
• 53 min
  13. UDP-glucuronosyltransferases

  • Prof. Abby Collier
• Phase II metabolizing enzymes: conjugating enzymes
• 31 min
  14. Glutathione transferases

  • Prof. Ralf Morgenstern
• 31 min
  15. Arylamine N-acetyltransferases 1

  • Prof. Edith Sim
• 23 min
  16. Arylamine N-acetyltransferases 2

  • Prof. Edith Sim
• 19 min
  17. Arylamine N-acetyltransferases 3

  • Prof. Edith Sim
• 56 min
  18. Methyltransferases

  • Prof. Richard Weinshilboum
• 22 min
  19. Amino acid conjugation: mechanism and enzymology

  • Dr. Kathleen Knights
• Clinical aspects
• 33 min
  20. Clinical significance of enzyme induction and inhibition

  • Prof. Kim Brøsen
• 39 min
  21. Clinical importance of pharmacogenetic polymorphisms affecting drug metabolism

  • Prof. Julia Stingl (formerly Kirchheiner)
• Latest Updates in the Field
• 34 min
  22. Mammalian flavin-containing monooxygenases

  • Prof. Allan Rettie
• Archived Lectures *These may not cover the latest advances in the field
• 54 min
  23. Glucuronidation and the UDP - glucuronosyltransferases

  • Prof. Peter Mackenzie
  • Prof. John Miners
• 38 min
  24. General factors affecting drug metabolism: the role of nuclear receptor superfamily members in induction

  • Dr. Patrick Maurel
• 28 min
  25. Catalytic cycle of cytochrome P450s

  • Prof. Gordon Roberts
• 40 min
  26. Drug metabolism and liver disease

  • Prof. Robert Branch
• 46 min
  27. Crystal structures of drug-metabolizing P450 monooxygenases

  • Prof. Eric Johnson
• 49 min
  28. Sulfation and human cytosolic sulfotransferases

  • Prof. Charles Falany
• 50 min
  29. Laboratory methods for the in vitro study of drug metabolism

  • Dr. Charles Crespi
• 45 min
  30. Clinical importance of pharmacogenetic polymorphisms affecting drug metabolism: psychopharmacology and pain

  • Prof. Julia Stingl (formerly Kirchheiner)
• 51 min
  31. Genetic variability in Paraoxonase 1 (PON1), an HDL associated esterase: impact on risk and pharmacokinetics

  • Res. Prof. Clement Furlong
• 53 min
  32. Pharmacogenomics

  • Prof. Magnus Ingelman-Sundberg

Printable Handouts

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Navigable Slide Index

1. Crystal structures of P450s
2. Structures of P450s
3. CYPs 3A4, 2A6 and 101
4. CYP2C5/diclofenac complex
5. Targeting of P450s to membranes
6. Microsomal P450s for crystall.
7. P450-membrane interactions
8. Proximal face of P450 2C5
9. Role of heme in O2 reduction
10. P450 heme binding site: CYP101 (1)
11. P450 heme binding site: CYP101 (2)
12. Substrate binding in CYP2C5
13. Family 2 P450s
14. P450s 2C8, 2C5 and 2A6
15. Comparison of CYP2C8/CYP2C5
16. Active site cavities - size/shape diff.
17. Active site shape and volume
18. Size discrimination
19. CYP2C5 - DFC vs. DMZ binding
20. DMZ/DFC complexes of CYP2C5
21. CYP2B4 - open/closed confo. (1)
22. CYP2B4 - open/closed confo. (2)
23. P450 flexibility
24. CYP2A6
25. Coumarin bound to CYP2A6
26. Substrate binding to P450s
27. CYP2C9 substrates
28. WT/mutant CYP2C9 conformations
29. CYP2C9 complexes - 1OG5/1R9O
30. Flurbiprofen contacts in CYP2C9
31. S-warfarin binding to CYP2C9
32. Small substrates - large active sites
33. Flurbiprofen complex of CYP2C9
34. CYP3A4 substrates
35. Structures of CYP 3A4 and 2C8
36. In silico docking of testosterone
37. CYP3A4 structures
38. Metyrapone bound to CYP3A4
39. Interfaces of CYP 2C8 and 3A4
40. CYP2C8 substrates
41. Montelukast bound to CYP2C8
42. Summary

Topics Covered

• Introduction to CYP450 architecture
• Shared structural features
• Catalytic mechanism
• Redox partner interactions
• Membrane topology
• Multiple modes of substrate binding and oxidation

Links

Series:

• Drug Metabolizing Enzymes

Categories:

• Biochemistry
• Metabolism & Nutrition
• Pharmaceutical Sciences

Therapeutic Areas:

• Cardiovascular & Metabolic

Talk Citation

Publication History

• Published on October 1, 2007
• Archived on November 17, 2016

Financial Disclosures

• Prof. Eric Johnson has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.