Discovery and development of purine-scaffold Hsp90 inhibitors Journal Article
| Authors: | Chiosis, G.; Kang, Y.; Sun, W. |
| Article Title: | Discovery and development of purine-scaffold Hsp90 inhibitors |
| Abstract: | The heat-shock protein 90 (Hsp90), an important target in cancer and other diseases, has become recently the focus of several drug discovery and development efforts. The initially identified natural-product inhibitors of Hsp90, such as geldanamycin, played a major role in elucidating its biological function and in determining its clinical relevance. Upcoming synthetic inhibitors, such as the purine-scaffold class, furthered our understanding on Hsp90 in cancer and neurodegenerative diseases and delivered what are promised to be clinical candidates with favorable pharmacologic profiles. This review intends to inform the reader on efforts ranging from the discovery of purine-scaffold Hsp90 inhibitors to their clinical translation as well as on their use as chemical tools to dissect the roles of Hsp90 in pathogenic systems. © 2008 informa UK Ltd. |
| Keywords: | protein kinase b; unclassified drug; clinical trial; review; doxorubicin; raf protein; nonhuman; drug targeting; unindexed drug; apoptosis; liver toxicity; protein degradation; etoposide; epidermal growth factor receptor; epidermal growth factor receptor 2; antineoplastic activity; cancer cell culture; drug structure; drug design; drug selectivity; drug synthesis; structure activity relation; drug dose escalation; cancer inhibition; drug research; heat shock protein 90 inhibitor; tanespimycin; heat shock protein 90; malignant neoplastic disease; down regulation; purine derivative; vinca alkaloid; drug bioavailability; anthracycline derivative; trastuzumab; drug binding site; antineoplastic antibiotic; adenosine triphosphatase; cell metabolism; drug protein binding; degenerative disease; drug stability; multidrug resistance; cytochrome p450; protein synthesis inhibition; neurodegeneration; geldanamycin; isoxazole derivative; ver 50589; hsp90; drug solubility; ansamycin derivative; cnf 2024; purine-scaffold; 17 dimethylethylamine 17 demethoxygeldanamycin; 8 benzothiazole purine derivative; 8 benzyl purine derivative; 8 phenylsulfanyl purine derivative; 9 benzyl purine derivative; acivicin; biib 021; colchicine derivative; protein mutl; drug classification |
| Journal Title: | Expert Opinion on Drug Discovery |
| Volume: | 3 |
| Issue: | 1 |
| ISSN: | 1746-0441 |
| Publisher: | Informa Healthcare |
| Date Published: | 2008-01-01 |
| Start Page: | 99 |
| End Page: | 114 |
| Language: | English |
| DOI: | 10.1517/17460441.3.1.99 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 12" - "Export Date: 17 November 2011" - "Source: Scopus" |
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