期刊
FRONTIERS IN BIOSCIENCE-LANDMARK
卷 17, 期 -, 页码 2269-2277出版社
FRONTIERS IN BIOSCIENCE INC
DOI: 10.2741/4050
关键词
Anticancer drugs; Geldanamycin; 17AAG; 17-DMAG; IPI-504; STA-9090; STA-1474; Radicicol; Novobiocin; Hsp90; Hsp90 inhibitors; Hsp90 client proteins; Review
资金
- Polish Ministry of Science and Higher Education [N N401 634140]
- College of Health, Beauty Care and Education in Poznan
The Hsp90 molecule, one of the most abundant heat shock proteins in mammalian cells, maintains homeostasis and prevents stress-induced cellular damage. Hsp90 is expressed under normal conditions at a level of about 1-2% of total proteins, while its expression increases 2-10 fold in cancer cells. The two main constitutively expressed isoforms of Hsp90 are known as Hsp90-alpha and Hsp90-beta, and their upregulation is associated with tumor progression, invasion and formation of metastases, as well as development of drug resistance. The Hsp90 is a key target for many newly established, potent anticancer agents containing Hsp90 N-terminal ATP binding inhibitors, such as geldanamycin, and its analogues 17AAG and 17DMAG. The therapeutic usage of geldanamycin has been limited due to its poor water solubility and severe hepatotoxicity. Therefore, its analogues, including 17AAG, 17DMAG, Tanespimycin and Retaspimycin hydrochloride, with improved pharmacokinetic profiles, have been developed.
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