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1. Introduction
2. Anticancer target: definition
3. Hsp90 - an ideal anti-cancer target?
4. Geldanamycin - discovery in phenotypic screen
5. Tumoricidal activity of ansamycins
6. Inhibition of Hsp90-pp60 complex formation
7. Hsp90-geldanamycin complex crystal structure
8. Geldanamycin blocks Hsp90 biological function
9. Mutant p53 requires functional Hsp90
10. Transformation-specific effects of Hsp90
11. Broad-spectrum effects of Hsp90
12. Hsp90 inhibition may affect many cancers
13. Hsp90 acts as a "buffer" of transformation
14. Are Hsp90 inhibitors a solution to cancer?
15. Tumor selectivity on Hsp90 inhibitors
16. Validation of Hsp90 as a target
17. Ansamycins
18. Improved formulations of 17-AAG (1)
19. Improved formulations of 17-AAG (2)
20. Pharmacodynamic markers
21. Radicicols
22. ADP inside Hsp90/kinase pocket
23. Purine-scaffold Hsp90 inhibitors (1)
24. PU3 mimics the biological effects of GM
25. Purine-scaffold Hsp90 inhibitors (2)
26. Pyrazole derivatives
27. Other Hsp90 inhibitors
28. Conclusions from small Hsp90 inhibitors use
29. Classical pharmacokinetic analysis relevance
30. Inhibition of Hsp90 - cytostatic or cytotoxic?
31. Limiting factors of anti-cancer potential (1)
32. Limiting factors of anti-cancer potential (2)
33. Limiting factors of anti-cancer potential (3)
34. Hsp90 inhibitors translation to other diseases
35. Concluding remarks

Topics Covered

• Heat shock protein 90 (Hsp90), a target in cancer
• Discovery of the first known Hsp90 inhibitor, geldanamycin
• Use of geldanamycin to understand the role of Hsp90 in malignant transformation
• Discovery of novel Hsp90 inhibitors
• Development and applications of Hsp90 inhibitors

Links

Series:

• Molecular Chaperones

Categories:

• Biochemistry
• Cancer
• Cell Biology

Therapeutic Areas:

• Oncology

Talk Citation

Publication History

• Published on October 1, 2007

Financial Disclosures

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