Published in Mol Cancer Ther on February 01, 2003
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17-AAG kills intracellular Leishmania amazonensis while reducing inflammatory responses in infected macrophages. PLoS One (2012) 0.84
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A mechanistic and structural analysis of the inhibition of the 90-kDa heat shock protein by the benzoquinone and hydroquinone ansamycins. Mol Pharmacol (2011) 0.83
Hsp90 regulates the phosphorylation and activity of serum- and glucocorticoid-regulated kinase-1. J Biol Chem (2008) 0.83
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The synthesis and evaluation of flavone and isoflavone chimeras of novobiocin and derrubone. Bioorg Med Chem (2009) 0.79
Heat shock proteins regulate activation-induced proteasomal degradation of the mature phosphorylated form of protein kinase C. J Biol Chem (2013) 0.78
Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors. Assay Drug Dev Technol (2013) 0.78
Could the Anti-Chaperone VER155008 Replace Temozolomide for Glioma Treatment. J Cancer (2015) 0.77
Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors. Bioorg Med Chem Lett (2009) 0.77
Protein Kinase Cα (PKCα) Is Resistant to Long Term Desensitization/Down-regulation by Prolonged Diacylglycerol Stimulation. J Biol Chem (2016) 0.75
Promoting Neuronal Tolerance of Diabetic Stress: Modulating Molecular Chaperones. Int Rev Neurobiol (2016) 0.75
Effectively delivering a unique hsp90 inhibitor using star polymers. ACS Med Chem Lett (2013) 0.75
Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay. Bioorg Med Chem Lett (2008) 0.75
Overcoming HSP27-mediated resistance by altered dimerization of HSP27 using small molecules. Oncotarget (2016) 0.75
mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res (2006) 18.44
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Heat shock factor 1 is a powerful multifaceted modifier of carcinogenesis. Cell (2007) 8.84
Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer. Cancer Cell (2011) 7.32
Targeting the dynamic HSP90 complex in cancer. Nat Rev Cancer (2010) 6.81
(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway. Proc Natl Acad Sci U S A (2009) 6.78
AKT inhibition relieves feedback suppression of receptor tyrosine kinase expression and activity. Cancer Cell (2011) 6.74
The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A (2010) 6.54
HIF overexpression correlates with biallelic loss of fumarate hydratase in renal cancer: novel role of fumarate in regulation of HIF stability. Cancer Cell (2005) 5.47
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The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells. Cancer Cell (2005) 4.48
4E-BP1 is a key effector of the oncogenic activation of the AKT and ERK signaling pathways that integrates their function in tumors. Cancer Cell (2010) 4.48
Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling. PLoS One (2008) 4.12
mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling. Cancer Discov (2011) 4.05
Drugging the cancer chaperone HSP90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress. Ann N Y Acad Sci (2007) 3.74
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 (2002) 3.72
Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function. J Biol Chem (2002) 3.70
Functional proteomic screens reveal an essential extracellular role for hsp90 alpha in cancer cell invasiveness. Nat Cell Biol (2004) 3.58
Chaperone-dependent E3 ubiquitin ligase CHIP mediates a degradative pathway for c-ErbB2/Neu. Proc Natl Acad Sci U S A (2002) 3.54
Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244). Cancer Res (2010) 3.54
IL-1beta-mediated up-regulation of HIF-1alpha via an NFkappaB/COX-2 pathway identifies HIF-1 as a critical link between inflammation and oncogenesis. FASEB J (2003) 3.37
Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas. Cancer Cell (2012) 3.37
Loss of PTEN/MMAC1/TEP in EGF receptor-expressing tumor cells counteracts the antitumor action of EGFR tyrosine kinase inhibitors. Oncogene (2003) 3.32
Heat shock protein 90 as a molecular target for cancer therapeutics. Cancer Cell (2003) 3.25
Tumor adaptation and resistance to RAF inhibitors. Nat Med (2013) 3.11
HSF1 drives a transcriptional program distinct from heat shock to support highly malignant human cancers. Cell (2012) 2.94
Mutant BRAF melanomas--dependence and resistance. Cancer Cell (2011) 2.87
Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study. J Clin Oncol (2007) 2.80
Tight coordination of protein translation and HSF1 activation supports the anabolic malignant state. Science (2013) 2.79
Rapid induction of apoptosis by PI3K inhibitors is dependent upon their transient inhibition of RAS-ERK signaling. Cancer Discov (2014) 2.79
CHIP activates HSF1 and confers protection against apoptosis and cellular stress. EMBO J (2003) 2.78
An acetylation site in the middle domain of Hsp90 regulates chaperone function. Mol Cell (2007) 2.75
Genetic predictors of MEK dependence in non-small cell lung cancer. Cancer Res (2008) 2.71
Imaging the pharmacodynamics of HER2 degradation in response to Hsp90 inhibitors. Nat Biotechnol (2004) 2.66
Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas. Cancer Discov (2013) 2.65
Resistance to BRAF inhibition in melanomas. N Engl J Med (2011) 2.58
Phase I trial of 17-allylamino-17-demethoxygeldanamycin in patients with advanced cancer. Clin Cancer Res (2007) 2.50
BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors. Cancer Discov (2012) 2.48
Selective inhibition of HER2-positive breast cancer cells by the HIV protease inhibitor nelfinavir. J Natl Cancer Inst (2012) 2.47
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors. Cancer Discov (2012) 2.47
HSP90 inhibition is effective in breast cancer: a phase II trial of tanespimycin (17-AAG) plus trastuzumab in patients with HER2-positive metastatic breast cancer progressing on trastuzumab. Clin Cancer Res (2011) 2.43
Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90. Nat Chem Biol (2011) 2.42
Harnessing Hsp90 function as a powerful, broadly effective therapeutic strategy for fungal infectious disease. Proc Natl Acad Sci U S A (2009) 2.35
Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2. Oncogene (2002) 2.34
Models from experiments: combinatorial drug perturbations of cancer cells. Mol Syst Biol (2008) 2.33
Phase I and pharmacologic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with solid tumors. J Clin Oncol (2005) 2.28
Fumarate hydratase deficiency in renal cancer induces glycolytic addiction and hypoxia-inducible transcription factor 1alpha stabilization by glucose-dependent generation of reactive oxygen species. Mol Cell Biol (2009) 2.27
Swe1Wee1-dependent tyrosine phosphorylation of Hsp90 regulates distinct facets of chaperone function. Mol Cell (2010) 2.24
Early tumor response to Hsp90 therapy using HER2 PET: comparison with 18F-FDG PET. J Nucl Med (2006) 2.24
Progression of RAS-mutant leukemia during RAF inhibitor treatment. N Engl J Med (2012) 2.19
Cyclin E amplification/overexpression is a mechanism of trastuzumab resistance in HER2+ breast cancer patients. Proc Natl Acad Sci U S A (2011) 2.18
Drug-induced ubiquitylation and degradation of ErbB receptor tyrosine kinases: implications for cancer therapy. EMBO J (2002) 2.17
Altered Hsp90 function in cancer: a unique therapeutic opportunity. Mol Cancer Ther (2004) 2.16
Development of new mouse lung tumor models expressing EGFR T790M mutants associated with clinical resistance to kinase inhibitors. PLoS One (2007) 2.14
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Targeting the molecular chaperone heat shock protein 90 provides a multifaceted effect on diverse cell signaling pathways of cancer cells. Clin Cancer Res (2007) 2.06
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Inhibition of heat shock protein 90 function down-regulates Akt kinase and sensitizes tumors to Taxol. Cancer Res (2003) 2.04
High levels of nuclear heat-shock factor 1 (HSF1) are associated with poor prognosis in breast cancer. Proc Natl Acad Sci U S A (2011) 2.03
mTORC1 inhibition is required for sensitivity to PI3K p110α inhibitors in PIK3CA-mutant breast cancer. Sci Transl Med (2013) 1.98
Small-molecule MAPK inhibitors restore radioiodine incorporation in mouse thyroid cancers with conditional BRAF activation. J Clin Invest (2011) 1.97
Extracellular heat shock protein 90: a role for a molecular chaperone in cell motility and cancer metastasis. Cancer Sci (2007) 1.96
BRAFV600E mutation is associated with preferential sensitivity to mitogen-activated protein kinase kinase inhibition in thyroid cancer cell lines. J Clin Endocrinol Metab (2008) 1.95
Threonine 22 phosphorylation attenuates Hsp90 interaction with cochaperones and affects its chaperone activity. Mol Cell (2011) 1.94
Phase II trial of 17-allylamino-17-demethoxygeldanamycin in patients with metastatic melanoma. Clin Cancer Res (2008) 1.94
Hsp90: a novel target for cancer therapy. Curr Top Med Chem (2006) 1.93
Clinical benefit of lapatinib-based therapy in patients with human epidermal growth factor receptor 2-positive breast tumors coexpressing the truncated p95HER2 receptor. Clin Cancer Res (2010) 1.92
Fitness trade-offs restrict the evolution of resistance to amphotericin B. PLoS Biol (2013) 1.88
A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants. Clin Cancer Res (2003) 1.83
Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation. Blood (2005) 1.83
Molecular diagnosis and therapy of kidney cancer. Annu Rev Med (2010) 1.82
Thyrotrophin receptor signaling dependence of Braf-induced thyroid tumor initiation in mice. Proc Natl Acad Sci U S A (2011) 1.82
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An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo. Cancer Biol Ther (2010) 1.77
PIK3CA mutation uncouples tumor growth and cyclin D1 regulation from MEK/ERK and mutant KRAS signaling. Cancer Res (2010) 1.77
Novobiocin: redesigning a DNA gyrase inhibitor for selective inhibition of hsp90. J Am Chem Soc (2006) 1.75
Inhibition of Hsp90 down-regulates mutant epidermal growth factor receptor (EGFR) expression and sensitizes EGFR mutant tumors to paclitaxel. Cancer Res (2008) 1.74
Simultaneous inhibition of hsp 90 and the proteasome promotes protein ubiquitination, causes endoplasmic reticulum-derived cytosolic vacuolization, and enhances antitumor activity. Mol Cancer Ther (2004) 1.72
Combinatorial drug design targeting multiple cancer signaling networks controlled by mitochondrial Hsp90. J Clin Invest (2009) 1.72
Hsp90 inhibitors identified from a library of novobiocin analogues. J Am Chem Soc (2005) 1.71
A combinatorial strategy for treating KRAS-mutant lung cancer. Nature (2016) 1.69
Histone deacetylases are required for androgen receptor function in hormone-sensitive and castrate-resistant prostate cancer. Cancer Res (2009) 1.68
Surface charge and hydrophobicity determine ErbB2 binding to the Hsp90 chaperone complex. Nat Struct Mol Biol (2005) 1.67
Cancer cells harboring MET gene amplification activate alternative signaling pathways to escape MET inhibition but remain sensitive to Hsp90 inhibitors. Cell Cycle (2009) 1.67
SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res (2008) 1.66
Identification of the genes for kidney cancer: opportunity for disease-specific targeted therapeutics. Clin Cancer Res (2007) 1.64
Hsp90: an emerging target for breast cancer therapy. Anticancer Drugs (2004) 1.64
A phase I study of 17-allylaminogeldanamycin in relapsed/refractory pediatric patients with solid tumors: a Children's Oncology Group study. Clin Cancer Res (2007) 1.61
Potential role of Hsp90 inhibitors in overcoming cisplatin resistance of bladder cancer-initiating cells. Int J Cancer (2011) 1.58
Hsp90-dependent activation of protein kinases is regulated by chaperone-targeted dephosphorylation of Cdc37. Mol Cell (2008) 1.57
Post-translational modifications of Hsp90 and their contributions to chaperone regulation. Biochim Biophys Acta (2011) 1.56
Hsp90 inhibition transiently activates Src kinase and promotes Src-dependent Akt and Erk activation. Proc Natl Acad Sci U S A (2006) 1.55
Actin microfilament aggregation induced by withaferin A is mediated by annexin II. Nat Chem Biol (2005) 1.55