Hsp90 inhibitors as novel cancer chemotherapeutic agents

Yufu, 1992, High constitutive expression of heat shock protein 90 ( in human acute leukemia cells, Leuk. Res., 16, 597, 10.1016/0145-2126(92)90008-U Xu, 1993, Heat-shock protein hsp90 governs the activity of pp60v-src kinase, Proc. Natl. Acad. Sci. U. S. A., 90, 7074, 10.1073/pnas.90.15.7074 Stancato, 1997, The hsp90-binding antibiotic geldanamycin decreases Raf levels and epidermal growth factor signaling without disrupting formation of signaling complexes or reducing the specific enzymatic activity of Raf kinase, J. Biol. Chem., 272, 4013, 10.1074/jbc.272.7.4013 Srivastava, 1991, Stress-induced proteins in immune response to cancer, Curr. Top. Microbiol. Immunol., 167, 109 Ciocca, 1992, Response of human breast cancer cells to heat shock and chemotherapeutic drugs, Cancer Res., 52, 3648 Whitesell, 1992, Benzoquinonoid ansamycins possess selective tumoricidal activity unrelated to src kinase inhibition, Cancer Res., 52, 1721 Whitesell, 1994, Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation, Proc. Natl. Acad. Sci. U. S. A., 91, 8324, 10.1073/pnas.91.18.8324 Ferrarini, 1992, Unusual expression and localization of heat-shock proteins in human tumor cells, Int. J. Cancer, 51, 613, 10.1002/ijc.2910510418 Blagosklonny, 1996, Mutant conformation of p53 translated in vitro or in vivo requires functional HSP90, Proc. Natl. Acad. Sci. U. S. A., 93, 8379, 10.1073/pnas.93.16.8379 Sato, 2000, Modulation of Akt kinase activity by binding to Hsp90, Proc. Natl. Acad. Sci. U. S. A., 97, 10832, 10.1073/pnas.170276797 Hostein, 2001, Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis, Cancer Res., 61, 4003 Schulte, 1996, Destabilization of Raf-1 by geldanamycin leads to disruption of the Raf-1–MEK–mitogen-activated protein kinase signalling pathway, Mol. Cell. Biol., 16, 5839, 10.1128/MCB.16.10.5839 An, 2000, The heat shock protein 90 antagonist geldanamycin alters chaperone association with p210bcr-abl and v-src proteins before their degradation by the proteasome, Cell Growth Differ., 11, 355 Shiotsu, 2000, Novel oxime derivatives of radicicol induce erythroid differentiation associated with preferential G(1) phase accumulation against chronic myelogenous leukemia cells through destabilization of Bcr-Abl with Hsp90 complex, Blood, 96, 2284, 10.1182/blood.V96.6.2284 Miller, 1994, Binding of benzoquinoid ansamycins to p100 correlates with their ability to deplete the erbB2 gene product p185, Biochem. Biophys. Res. Commun., 201, 1313, 10.1006/bbrc.1994.1847 Miller, 1994, Depletion of the erbB-2 gene product p185 by benzoquinoid ansamycins, Cancer Res., 54, 2724 Chavany, 1996, p185erbB2 binds to GRP94 in vivo. Dissociation of the p185erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of p185erbB2, J. Biol. Chem., 271, 4974, 10.1074/jbc.271.9.4974 Stepanova, 1996, Mammalian p50Cdc37 is a protein kinase-targeting subunit of Hsp90 that binds and stabilizes Cdk4, Genes Dev., 10, 1491, 10.1101/gad.10.12.1491 Aligue, 1994, A role for Hsp90 in cell cycle control: Wee1 tyrosine kinase activity requires interaction with Hsp90, EMBO J., 13, 6099, 10.1002/j.1460-2075.1994.tb06956.x Minet, 1999, Hypoxia-induced activation of HIF-1: role of HIF-1α–Hsp90 interaction, FEBS Lett., 460, 251, 10.1016/S0014-5793(99)01359-9 Fang, 1996, Hsp90 regulates androgen receptor hormone binding affinity in vivo, J. Biol. Chem., 271, 28697, 10.1074/jbc.271.45.28697 Segnitz, 1997, The function of steroid hormone receptors is inhibited by the hsp90-specific compound geldanamycin, J. Biol. Chem., 272, 18694, 10.1074/jbc.272.30.18694 Bagatell, 2001, Destabilization of steroid receptors by heat shock protein 90-binding drugs: a ligand-independent approach to hormonal therapy of breast cancer, Clin. Cancer Res., 7, 2076 Haendler, 2001, Androgen receptor signalling: comparative analysis of androgen response elements and implication of heat-shock protein 90 and 14-3-3eta, Mol. Cell. Endocrinol., 173, 63, 10.1016/S0303-7207(00)00434-2 Holt, 1999, Functional requirement of p23 and Hsp90 in telomerase complexes, Genes Dev., 13, 817, 10.1101/gad.13.7.817 Grenert, 1997, The amino-terminal domain of heat shock protein 90 (hsp90) that binds geldanamycin is an ATP/ADP switch domain that regulates hsp90 conformation, J. Biol. Chem., 272, 23843, 10.1074/jbc.272.38.23843 Stebbins, 1997, Crystal structure of an Hsp90–geldanamycin complex: targeting of a protein chaperone by an antitumor agent, Cell, 89, 239, 10.1016/S0092-8674(00)80203-2 Prodromou, 1997, Identification and structural characterization of the ATP/ADP-binding site in the Hsp90 molecular chaperone, Cell, 90, 65, 10.1016/S0092-8674(00)80314-1 Scheibel, 1998, The Hsp90 complex – a super-chaperone machine as a novel drug target, Biochem. Pharmacol., 56, 675, 10.1016/S0006-2952(98)00120-8 Schneider, 1996, Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90, Proc. Natl. Acad. Sci. U. S. A., 93, 14536, 10.1073/pnas.93.25.14536 Connell, 2001, The co-chaperone CHIP regulates protein triage decisions mediated by heat-shock proteins, Nat. Cell Biol., 3, 93, 10.1038/35050618 Meacham, 2001, The Hsc70 co-chaperone CHIP targets immature CFTR for proteasomal degradation, Nat. Cell Biol., 3, 100, 10.1038/35050509 Chiosis, 2001, LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family, Bioorg. Med. Chem. Lett., 11, 909, 10.1016/S0960-894X(01)00099-3 Schulte, 1998, The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin, Cancer Chemother. Pharmacol., 42, 273, 10.1007/s002800050817 Kelland, 1999, DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90, J. Natl. Cancer Inst., 91, 1940, 10.1093/jnci/91.22.1940 Agnew, 2001, Measurement of the novel antitumor agent 17-(allylamino)-17-demethoxygeldanamycin in human plasma by high-performance liquid chromatography, J. Chromatogr. B Biomed. Sci. Appl., 755, 237, 10.1016/S0378-4347(01)00113-X Srethapakdi, 2000, Inhibition of Hsp90 function by ansamycins causes retinoblastoma gene product-dependent G1 arrest, Cancer Res., 60, 3940 Nimmanapalli, 2001, Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts, Cancer Res., 61, 1799 Solit, D. et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts. Clin. Cancer Res. (in press) Blagosklonny, 2001, The Hsp90 inhibitor geldanamycin selectively sensitizes Bcr-Abl-expressing leukemia cells to cytotoxic chemotherapy, Leukemia, 15, 1537, 10.1038/sj.leu.2402257 Gorre, 2001, Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification, Science, 293, 876, 10.1126/science.1062538 Munster, 2001, Modulation of Hsp90 function by ansamycins sensitizes breast cancer cells to chemotherapy-induced apoptosis in an RB- and schedule-dependent manner, Clin. Cancer Res., 7, 2155 Sausville, 2001, Combining cytotoxics and 17-allylamino, 17-demethoxygeldanamycin: sequence and tumor biology matters, Clin Cancer Res., 7, 2228 Nguyen, D.M. et al. (2001) Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis. Ann. Thorac. Surg. 72, 371–378, discussion 378–379. Nguyen, 1999, Sequence-dependent enhancement of paclitaxel toxicity in non-small cell lung cancer by 17-allylamino 17-demethoxygeldanamycin, J. Thorac. Cardiovasc. Surg., 118, 908, 10.1016/S0022-5223(99)70061-9 Horowitz, 1990, Frequent inactivation of the retinoblastoma anti-oncogene is restricted to a subset of human tumor cells, Proc. Natl. Acad. Sci. U. S. A., 87, 2775, 10.1073/pnas.87.7.2775 Lai, 1995, Molecular genetic characterization of neuroendocrine lung cancer cell lines, Anticancer Res., 15, 225 Zhong, 1999, Overexpression of hypoxia-inducible factor 1α in common human cancers and their metastases, Cancer Res., 59, 5830 Kurose, 2001, Frequent loss of PTEN expression is linked to elevated phosphorylated Akt levels, but not associated with p27 and cyclin D1 expression, in primary epithelial ovarian carcinomas, Am. J. Pathol., 158, 2097, 10.1016/S0002-9440(10)64681-0 Sharma, 1998, Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol, Oncogene, 16, 2639, 10.1038/sj.onc.1201790 Schulte, 1998, Antibiotic radicicol binds to the N-terminal domain of Hsp90 and shares important biologic activities with geldanamycin, Cell Stress Chaperones, 3, 100, 10.1379/1466-1268(1998)003<0100:ARBTTN>2.3.CO;2 Roe, 1999, Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin, J. Med. Chem., 42, 260, 10.1021/jm980403y Marcu, 2000, The heat shock protein 90 antagonist novobiocin interacts with a previously unrecognized ATP-binding domain in the carboxyl terminus of the chaperone, J. Biol. Chem., 275, 37181, 10.1074/jbc.M003701200 Marcu, 2000, Novobiocin and related coumarins and depletion of heat shock protein 90-dependent signaling proteins, J. Natl. Cancer Inst., 92, 242, 10.1093/jnci/92.3.242 Chiosis, 2001, A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells, Chem. Biol., 8, 289, 10.1016/S1074-5521(01)00015-1 Slepian, 1996, Pre-conditioning of smooth muscle cells via induction of the heat shock response limits proliferation following mechanical injury, Biochem. Biophys. Res. Commun., 225, 600, 10.1006/bbrc.1996.1217 Conde, 1997, Induction of heat shock proteins by tyrosine kinase inhibitors in rat cardiomyocytes and myogenic cells confers protection against simulated ischemia, J. Mol. Cell. Cardiol., 29, 1927, 10.1006/jmcc.1997.0431 Mimnaugh, 1995, Possible role for serine/threonine phosphorylation in the regulation of the heteroprotein complex between the hsp90 stress protein and the pp60v-src tyrosine kinase, J. Biol. Chem., 270, 28654, 10.1074/jbc.270.48.28654 Zhao, 2001, Hsp90 phosphorylation is linked to its chaperoning function. Assembly of the reovirus cell attachment protein, J. Biol. Chem., 276, 32822, 10.1074/jbc.M105562200 Rutherford, 1998, Hsp90 as a capacitor for morphological evolution, Nature, 396, 336, 10.1038/24550