• An Overview of Drug Discovery and Development
• 78 min
  1. Rules and filters and their impact on success in chemical biology and drug discovery

  • Dr. Christopher Lipinski
• 37 min
  2. Where did drugs come from?

  • Dr. David Swinney
• Target Selection in Early Stage Drug Discovery
• 42 min
  3. G-Protein coupled receptors in drug discovery

  • Dr. Mark Wigglesworth
• 42 min
  4. Enzymology in drug discovery 1

  • Prof. Robert Copeland
• 66 min
  5. Enzymology in drug discovery 2

  • Prof. Robert Copeland
• 41 min
  6. Inhibiting protein-protein interactions 1

  • Dr. Adrian Whitty
• 35 min
  7. Inhibiting protein-protein interactions 2

  • Dr. Adrian Whitty
• Key Drug Discovery Challenges in Major Therapeutic Areas
• 64 min
  8. Current trends in antiviral drug development

  • Prof. Dr. Erik De Clercq
• 27 min
  9. The challenge of developing drugs for neglected parasitic diseases

  • Prof. James Mckerrow
• 55 min
  10. Is there a role for academia in drug discovery

  • Dr. Adrian J. Ivinson
• 31 min
  11. Key drug discovery challenges in cardiovascular medicine

  • Dr. Dan Swerdlow
  • Dr. Michael V. Holmes
• Methods of Hit Identification
• 46 min
  12. Fragment-based lead discovery

  • Dr. Daniel A. Erlanson
• Medicinal Chemistry and SAR
• 53 min
  13. Hit to lead

  • Dr. Michael Rafferty
• 37 min
  14. Prodrug strategies to overcome problems in drug therapy

  • Prof. Jarkko Rautio
• 40 min
  15. Deep ocean microorganisms yield mechanistically-novel anticancer agents

  • Prof. William Fenical
• From Lead to Drug
• 25 min
  16. Biomarkers in drug development: potential use and challenges

  • Dr. Abdel-Bassett Halim
• Case Studies in Drug Discovery
• 35 min
  17. Current concepts for the management of patients with osteoporosis

  • Dr. Michael Lewiecki
• 35 min
  18. Discovery of Levetiracetam (Keppra(R)): The first SV2A ligand for the treatment of epilepsy

  • Dr. Henrik Klitgaard
• 36 min
  19. Teixobactin kills pathogens without detectable resistance

  • Prof. Kim Lewis
• 20 min
  20. Discovery of schizophrenia drug targets from DISC1 mechanisms

  • Prof. Atsushi Kamiya
• Archived Lectures *These may not cover the latest advances in the field
• 46 min
  21. CNS-drug design

  • Prof. Quentin Smith
• 38 min
  22. Imatinib as a paradigm of targeted cancer therapies

  • Prof. Brian Druker
• 44 min
  23. New and emerging treatments for osteoporosis

  • Dr. Michael Lewiecki
• 38 min
  24. Prodrugs and drug delivery

  • Prof. Jarkko Rautio

Printable Handouts

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Navigable Slide Index

1. Introduction
2. Earth is 70% ocean and 70% ocean bottom!
3. How can we access the deep ocean systems?
4. Deep ocean sediment sampling
5. Unknown actinomycete bacteria cultivated
6. New phylogenetic diversity: marine actinomycetes
7. Bioactive marine microbial metabolites
8. Problems with marine microbial drug discovery
9. Three species of Salinispora recognized
10. Chemical study - Salinispora tropica CNB-440
11. Salinosporamide A, a potent anticancer agent
12. Sal A proteasome enzymatic specificity
13. Sal A reactivity during binding to 20S proteasome
14. Ammosamides A and B - Mar 14 group
15. Ammosamides A and B
16. Ammosamides A and B cancer bioactivities
17. Cell cycle response to ammosamide B
18. Protein target of ammosamide B
19. Protein target of ammosamide B is myosin II
20. X-ray structure of myosin II
21. Predicted myosin II binding site (docking studies)
22. The MAR 4 actinomycetes - Streptomycetaceae
23. The MAR 4 actinomycetes metabolites
24. Napyradiomycins induce rapid cytotoxicity
25. Napyradiomycins and apoptosis in HCT-116 cells
26. Preparation of fluorescent coumarin derivatives
27. Two MAR 4 probes bind to the ER in HeLa cells
28. Immunoprecipitation leads to “Grp94” as target
29. Role of the Hsp90 proteins in cell regulation
30. Streptomyces strain CNH-287, a new species
31. X-ray structure of chlorizidine A
32. Reactivity of chlorizidine A
33. Synthesis of the chlorizidine A fluorescent probe
34. Incubation of chlorizidine A probe & HCT-116 cells
35. Immunoprecipitation leads to ID of ENO1
36. Crystal structure of human enolase 1
37. Concluding remarks
38. Acknowledgements

Topics Covered

• Structurally unprecedented marine bacterial metabolites
• Developing new molecules for the treatment of cancer
• Discovery of the protein targets of apoptosis-inducing metabolites
• Developing the potential of natural products to treat cancer by alternative mechanisms of action
• Discoveries of GRP94, myosin II and related cellular proteins as targets of new cytotoxins

Links

Series:

• Small Molecule Drug Discovery

Categories:

• Cancer
• Microbiology
• Pharmaceutical Sciences

Therapeutic Areas:

• Oncology

Talk Citation

Publication History

• Published on September 23, 2013
• Reviewed on September 23, 2021

Financial Disclosures

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