• 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

PDF

Navigable Slide Index

1. In vitro study of drug metabolism
2. Lecture overview (1)
3. Lecture overview (2)
4. Subcellular fractionation
5. Hepatocyte isolation
6. Classes of drug metab. enzymes
7. Location of metabolic enzymes
8. Enzyme cofactor requirements
9. Conducting in vitro assays
10. Performing assays - aspects (1)
11. Performing assays - aspects (2)
12. Performing assays - aspects (3)
13. Common applications
14. Metabolite formation kinetics
15. BFC, BQ, CYP1A2 and CYP3A4
16. Metabolic stability
17. Metabolic stability in humans
18. Reaction phenotyping
19. Indep. experimental approaches
20. cDNA-expressed enzymes
21. Correlation approach
22. Enzyme selective inhibitors
23. Inhibitor depletion
24. CYP probe substrates/inhibitors
25. Enzyme inhibition analysis
26. CYP enzymes for drug metabolism
27. Types of enzyme inhibition
28. In vitro competitive inhibition
29. Layout for IC50
30. Example IC50 curves
31. Substrate dependent differences
32. Mechanism-based inhibition
33. Measuring MBI parameters
34. Effect of pre-incubation w/ NADPH
35. Enzyme inhibition results
36. Enzyme inhibition in vivo
37. Conclusions
38. Thank you

Topics Covered

• Major classes of DMEs
• Systems for laboratory study
• Practical aspects
• Examples of application
• Obtaining high quality data
• Minimizing artefacts

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 October 29, 2018

Financial Disclosures

• Dr. Charles Crespi has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.