Emerging Hsp90 inhibitors: From discovery to clinic Journal Article
| Authors: | Chiosis, G.; Rodina, A.; Moulick, K. |
| Article Title: | Emerging Hsp90 inhibitors: From discovery to clinic |
| Abstract: | Hsp90 is a chaperone with important roles in maintaining transformation and in elevating the survival and growth potential of cancer cells. Activation of signaling pathways mediated by Hsp90 protein clients is necessary for cell proliferation, regulation of cell cycle progression and apoptosis. Additionally, gain-of-function mutations responsible for transformation often require Hsp90 for the maintenance of their folded, functionally active conformations. These characteristics promise Hsp90 as an important target in cancer therapy and prompt for the identification, development and clinical translation of small molecule inhibitors of the chaperone. This review intends to update the reader on the status of several existing and emerging classes of direct inhibitors of Hsp90 ATPase activity. © 2006 Bentham Science Publishers Ltd. |
| Keywords: | signal transduction; unclassified drug; gene mutation; clinical trial; review; cancer growth; nonhuman; antineoplastic agents; drug targeting; antineoplastic agent; protein conformation; cell proliferation; metabolism; cell survival; cell cycle progression; unindexed drug; apoptosis; bortezomib; enzyme inhibition; liver toxicity; classification; protein binding; adenosine diphosphate; drug design; cancer therapy; drug antagonism; cell transformation; pyrazole derivative; cancer cell; heat shock protein 90 inhibitor; heat shock protein 90; drug clearance; hsp90 heat-shock proteins; purine derivative; adenosine triphosphate; protein folding; natural product; pyrimidine derivative; malignant transformation; antineoplastic antibiotic; adenosine triphosphatase; adenosine triphosphatases; protein inhibitor; geldanamycin; oxime derivative; pochonin d; chaperone; pyrazolopyrimidine derivative; ansamycin derivative; g 3130; pu 3; 17 allylamino 17 demethoxygeldanamycin; shepherdin; ver 49009; cct 018159; ipi 504; pu-class hsp90 inhibitors; radicicol and derivatives; kf 55823; pyrrolopyrimidine derivative; 17aag; 17dmag; 3,4-diarylpyrazoles; anti-cancer therapeutics; pu 24fc1; pu h 58; radidicol; rbt 0028535 |
| Journal Title: | Anti-Cancer Agents in Medicinal Chemistry |
| Volume: | 6 |
| Issue: | 1 |
| ISSN: | 1871-5206 |
| Publisher: | Bentham Science Publishers |
| Date Published: | 2006-01-01 |
| Start Page: | 1 |
| End Page: | 8 |
| Language: | English |
| PUBMED: | 16475922 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 26" - "Export Date: 4 June 2012" - "Source: Scopus" |
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