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Cancer Therapy
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BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance
Article first published online: 12 AUG 2009
DOI: 10.1002/ijc.24825
Copyright © 2009 UICC
Additional Information
How to Cite
Zhang, H., Neely, L., Lundgren, K., Yang, Y.-C., Lough, R., Timple, N. and Burrows, F. (2010), BIIB021, a synthetic Hsp90 inhibitor, has broad application against tumors with acquired multidrug resistance. Int. J. Cancer, 126: 1226–1234. doi: 10.1002/ijc.24825
Publication History
- Issue published online: 27 DEC 2009
- Article first published online: 12 AUG 2009
- Accepted manuscript online: 12 AUG 2009 12:00AM EST
- Manuscript Accepted: 30 JUL 2009
- Manuscript Received: 12 MAR 2009
References
- 1, , , , , , , , , , , , et al. Development of 17-allylamino-17-demethoxygeldanamycin hydroquinone hydrochloride (IPI-504), an anti-cancer agent directed against Hsp90. Proc Natl Acad Sci USA 2006; 103: 17408–13.
- 2, , , , , , . In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative. Cancer Chemother Pharmacol 2005; 56: 115–25.
- 3, , . Multidrug resistance in cancer: role of ATP-dependent transporters. Nat Rev Cancer 2002; 2: 48–58.
- 4, , . Resistance mechanisms associated with altered intracellular distribution of anticancer agents. Pharmacol Therapeut 2000; 85: 217–29.
- 5, , , , , . Expression of a multidrug-resistance gene in human tumors and tissues. Proc Natl Acad Sci USA 1987; 84: 265–9.
- 6, , , . P-glycoprotein: from genomics to mechanism. Oncogene 2003; 22: 7468–85.
- 7, , , , . Distribution of STI-571 to the brain is limited by P-glycoprotein-mediated efflux. J Pharmacol Exp Ther 2003; 304: 1085–92.
- 8, , , . The role of ABC transporters in drug resistance, metabolism and toxicity. Curr Drug Deliv 2004; 1: 27–42.
- 9, , , . P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res 2003; 48: 347–59.
- 10. P-glycoprotein-mediated efflux as a major factor in the variance of absorption and distribution of drugs: modulation of chemotherapy resistance. Methods Find Exp Clin Pharmacol 2002; 24: 501–14.
- 11, , . Efflux transporters and their clinical relevance. Mini Rev Med Chem 2005; 5: 183–95.
- 12, , , , . MDR1 and MRP expression in chronic B-cell lymphoproliferative disorders. Br J Haematol 1998; 102: 710–7.
- 13, . Redundancy of biological regulation as the basis of emergence of multidrug resistance. Int Rev Cytol 2005; 246: 1–29.
- 14, , , , . DT-diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90. J Natl Cancer Inst 1999; 91: 1940–9.
- 15, , , , , . Regulation of 17-AAG-induced apoptosis: role of Bcl-2, Bcl-XL and Bax downstream of 17-AAG-mediated down-regulation of Akt, Raf-1, and Src kinases. Blood 2003; 102: 269–75.
- 16, , , , , . Formation of 17-allylamino-demethoxygeldanamycin (17-AAG) hydroquinone by NAD(P)H:quinone oxidoreductase 1: role of 17-AAG hydroquinone in heat shock protein 90 inhibition. Cancer Res 2005; 65: 10006–15.
- 17Process for preparing 17-allyl amino geldanamycin (17-AAG) and other ansamycins. Pat, no. WO 0,302,6571. 2002.
- 18, , , , , , , , , , , , et al. Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity. J Med Chem 2007; 50: 2767–78.
- 19. P-glycoprotein as a drug target in the treatment of multidrug resistant cancer. Curr Drug Targets 2000; 1: 85–99.
- 20, , . Multidrug resistance in a human small cell lung cancer cell line selected in adriamycin. Cancer Res 1987; 47: 2594–8.
- 21, , , , , , , , . Loss of multidrug resistance protein 1 expression and folate efflux activity results in a highly concentrative folate transport in human leukemia cells. J Biol Chem 2003; 278: 6680–6.
- 22, , , . Reversal of multidrug resistance-associated protein-mediated daunorubicin resistance by camptothecin. J Pharm Sci 2002; 91: 1765–75.
- 23, , , , . Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis. Cancer Res 2001; 61: 4003–9.
- 24, , , . Inhibition of Hsp90 function by ansamycins causes retinoblastoma gene product-dependent G1 arrest. Cancer Res 2000; 60: 3940–6.
- 25, . HSP90 as a new therapeutic target for cancer therapy: the story unfolds. Expert Opin Biol Ther 2002; 2: 3–24.
- 26, . Heat shock protein 90. Curr Opin Oncol 2003; 15: 419–24.
- 27, . Targeting multiple signal transduction pathways through inhibition of Hsp90. J Mol Med 2004; 82: 488–99.
- 28, . Hsp90: a novel target for cancer therapy. Curr Topics Med Chem 2006; 6: 1205–14.
- 29, , , , , , , , , , , , et al. Phase I trial of 17-allylamino-17-demethoxygeldanamycin in patients with advanced cancer. Clin Cancer Res 2007; 13: 1775–82.
- 30, , , . Hsp90 inhibitors in the clinic. Handb Exp Pharmacol 2006: 331–58.
- 31, , . Clinical development of 17-allylamino, 17-demethoxygeldanamycin. Curr Cancer Drug Targets 2003; 3: 377–83.
- 32, , , , , , , . A phase II trial of 17-(allylamino)-17-demethoxygeldanamycin in patients with papillary and clear cell renal cell carcinoma. Invest New Drugs 2006; 24: 543–6.
- 33, , , , , , , , , , , , et al. A phase II trial of 17-allylamino-17-demethoxygeldanamycin in patients with hormone-refractory metastatic prostate cancer. Clin Cancer Res 2008; 14: 7940–6.
- 34, , , , . Anticancer multidrug resistance mediated by MRP1: recent advances in the discovery of reversal agents. Med Res Rev 2005; 25: 453–72.
- 35, , , , , , . The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Cancer Res 2005; 65: 2577–82.
- 36, , , , , , , . P-glycoprotein-mediated resistance to Hsp90-directed therapy is eclipsed by the heat shock response. Cancer Res 2008; 68: 7419–27.
- 37, , , , , , , , , , , , et al. BIIB021, an orally available, small molecule inhibitor of the heat shock protein, Hsp90. Mol Cancer Ther 2009; 8: 921–9.

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