Targeting Hsp90: Small-molecule inhibitors and their clinical development Journal Article
| Authors: | Taldone, T.; Gozman, A.; Maharaj, R.; Chiosis, G. |
| Article Title: | Targeting Hsp90: Small-molecule inhibitors and their clinical development |
| Abstract: | The Hsp90 multichaperone complex has important roles in the development and progression of malignant transformation. Several small-molecule inhibitors of Hsp90 of diverse chemotypes have shown potent antitumor activity in a wide-range of malignancies, and are currently in clinical or late-stage preclinical investigation. This review intends to update the reader on advances made over the past two years in the clinical development of Hsp90 inhibitors in advanced cancers. It will refer to the two 17-AAG formulations, tanespimycin and IPI-504, and to synthetic small molecules, among which are the purine-scaffold Hsp90 inhibitor CNF2024/BIIB021, the isoxazole derivative VER-52296/NVP-AUY922, and the carbazol-4-one benzamide derivative SNX-5422, and will present our current knowledge on their clinical performance. © 2008 Elsevier Ltd. All rights reserved. |
| Keywords: | unclassified drug; acute granulocytic leukemia; clinical trial; drug tolerability; review; advanced cancer; monotherapy; side effect; unspecified side effect; antineoplastic agents; drug targeting; antineoplastic agent; neoplasm; animals; gastrointestinal stromal tumor; low drug dose; melanoma; bortezomib; liver toxicity; multiple myeloma; breast cancer; neuropathy; combination chemotherapy; antineoplastic activity; drug potency; drug structure; cancer resistance; drug dose escalation; drug research; drug response; 17 demethoxy 17 (2 dimethylaminoethylamino)geldanamycin; heat shock protein 90 inhibitor; tanespimycin; heat shock protein 90; hsp90 heat-shock proteins; heat shock protein 70; trastuzumab; antibiotics, antineoplastic; malignant transformation; drug delivery system; benzoquinones; lactams, macrocyclic; drug formulation; tanespimycin hydroquinone; kos 1022; nvp auy 922; snx 5422; cnf 2024; biib 021; cremophor; snx 2122; sta 9090; ver 52296 |
| Journal Title: | Current Opinion in Pharmacology |
| Volume: | 8 |
| Issue: | 4 |
| ISSN: | 1471-4892 |
| Publisher: | Elsevier Inc. |
| Date Published: | 2008-08-01 |
| Start Page: | 370 |
| End Page: | 374 |
| Language: | English |
| DOI: | 10.1016/j.coph.2008.06.015 |
| PUBMED: | 18644253 |
| PROVIDER: | scopus |
| PMCID: | PMC2760289 |
| DOI/URL: | |
| Notes: | --- - "Cited By (since 1996): 108" - "Export Date: 17 November 2011" - "CODEN: COPUB" - "Source: Scopus" |
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