• 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. Introduction
2. Human NAT1: overview
3. NAT1 specific ligands
4. Screening for NAT substrates & inhibitors
5. Biomarker detection in breast cancer (1)
6. Biomarker detection in breast cancer (2)
7. A single binding site
8. Naphthoquinone inhibits acetylation activity
9. Naphthoquinone 1 inhibits AcCoA hydrolysis
10. R127 mutation blocks inhibition by naphthoquinone
11. R127 in hNAT1 and mNAT2
12. Improving NAT1 detection
13. NAT1 knock-down alters cell growth & survival
14. Status of NAT1 research
15. Arylamine N-acetyltransferases (recap)
16. Nat in fungi metabolise anti-fungal toxin
17. Activity of fungal Nat enzymes
18. Nat in prokaryotes including mycobacteria
19. Prokaryotic Nats
20. Active site of Mycobacterium smegmatis Nat
21. Active site of Pseudomonas aerogunosa Nt
22. Life cycle of M. tuberculosis
23. Return to N-acetylation of isoniazid (INH)
24. KatG and Nat
25. Nats in prokaryotes
26. Nats affect lipid levels in cells
27. M. bovis BCG phenotype in nat KO cells (1)
28. M. bovis BCG phenotype in nat KO cells (2)
29. M. bovis BCG phenotype in nat KO cells (3)
30. M. bovis BCG phenotype in nat KO cells (4)
31. Inhibiting Nat and mycolic acid
32. Summary: alteration of nat expression
33. Mycobacterial Nat specific ligands
34. Detecting Nat substrates & inhibitors
35. Mycobacterial Nat inhibitors identified from screen
36. Nat as an anti-tubercular target
37. Triazole vs. mycobacteria
38. Growth inside macrophage is affected
39. Synthetic analogues of 190
40. Docking the compound into the active site of Nat
41. Piperidinol inhibition of mycobacterial Nat
42. Inhibition by piperidinol
43. Piperidinol in the presence of mycobacterial Nat
44. Binding of piperidinol fragment
45. Structure of TB Nat now available
46. TB Nat inhibitors
47. Summary: chemical inhibition
48. The future
49. Acknowledgments

Topics Covered

• Mechanism of action
• Reaction substrates
• Isoform substrate profiles
• Isoenzymes NAT1 and NAT2
• Regulation of gene expression
• Pharmacogenetics
• Phenotype/genotype correlation
• Ethnic variation
• Transgenic mouse models
• NAT protein structures
• NAT as a biomarker in breast cancer
• NAT inhibitors as diagnostic agents
• NAT in mycobacteria
• NAT inhibitors as an approach to potential anti-tubercular agents

Links

Series:

• Drug Metabolizing Enzymes

Categories:

• Biochemistry
• Metabolism & Nutrition
• Pharmaceutical Sciences

Therapeutic Areas:

• Cardiovascular & Metabolic

Talk Citation

Publication History

• Published on October 1, 2007
• Updated on July 28, 2016

Financial Disclosures

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