Published in Bioorg Med Chem Lett on October 05, 2005
Discovery and development of heat shock protein 90 inhibitors. Bioorg Med Chem (2008) 1.36
Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells. Cancer Res (2009) 1.34
High-throughput assay for the identification of Hsp90 inhibitors based on Hsp90-dependent refolding of firefly luciferase. Bioorg Med Chem (2007) 1.11
Different poses for ligand and chaperone in inhibitor-bound Hsp90 and GRP94: implications for paralog-specific drug design. J Mol Biol (2009) 1.06
The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis. J Mol Biol (2015) 0.98
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Identification, design and bio-evaluation of novel Hsp90 inhibitors by ligand-based virtual screening. PLoS One (2013) 0.77
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Ethyl 5-(ethoxy-carbon-yl)-3-(4-methoxy-phen-yl)-1H-pyrazole-1-acetate. Acta Crystallogr Sect E Struct Rep Online (2007) 0.77
Synthesis, characterization, and pharmacological evaluation of novel azolo- and azinothiazinones containing 2,4-dihydroxyphenyl substituent as anticancer agents. Monatsh Chem (2015) 0.75
Molecular docking and pharmacophore studies of heterocyclic compounds as Heat shock protein 90 (Hsp90) Inhibitors. Bioinformation (2016) 0.75
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Activation of the ATPase activity of hsp90 by the stress-regulated cochaperone aha1. Mol Cell (2002) 3.89
Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies. J Clin Oncol (2005) 3.42
Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises. Curr Opin Pharmacol (2008) 3.41
The Hsp90 molecular chaperone: an open and shut case for treatment. Biochem J (2008) 3.33
Combinatorial drug therapy for cancer in the post-genomic era. Nat Biotechnol (2012) 3.10
Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Cancer Res (2007) 3.09
NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res (2008) 2.76
Inhibitors of the HSP90 molecular chaperone: current status. Adv Cancer Res (2006) 2.55
HSP90 as a new therapeutic target for cancer therapy: the story unfolds. Expert Opin Biol Ther (2002) 2.53
Dual targeting of HSC70 and HSP72 inhibits HSP90 function and induces tumor-specific apoptosis. Cancer Cell (2008) 2.49
Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol Cancer Ther (2009) 2.43
Heat shock protein inhibition is associated with activation of the unfolded protein response pathway in myeloma plasma cells. Blood (2007) 2.38
Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin. Cancer Res (2005) 2.34
New approaches to molecular cancer therapeutics. Nat Chem Biol (2006) 2.28
Inhibitors of the heat shock response: biology and pharmacology. FEBS Lett (2007) 2.21
Targeting of multiple signalling pathways by heat shock protein 90 molecular chaperone inhibitors. Endocr Relat Cancer (2006) 2.11
A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding. EMBO Rep (2008) 2.09
A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription. Cancer Res (2010) 2.05
Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. J Med Chem (2010) 2.04
Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma. Cell Cycle (2009) 1.96
Histone H3.3. mutations drive pediatric glioblastoma through upregulation of MYCN. Cancer Discov (2013) 1.93
ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system. Nat Chem Biol (2013) 1.90
A public-private partnership to unlock the untargeted kinome. Nat Chem Biol (2013) 1.83
Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms. Chem Biol (2004) 1.80
Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models. Clin Cancer Res (2005) 1.78
Targeting HSP70: the second potentially druggable heat shock protein and molecular chaperone? Cell Cycle (2010) 1.75
A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cells. Cancer Chemother Pharmacol (2009) 1.72
Pharmacodynamic biomarkers for molecular cancer therapeutics. Adv Cancer Res (2007) 1.71
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem (2007) 1.67
Envisioning the future of early anticancer drug development. Nat Rev Cancer (2010) 1.67
Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin. Cancer Res (2007) 1.66
Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem (2006) 1.62
A phase I study of the heat shock protein 90 inhibitor alvespimycin (17-DMAG) given intravenously to patients with advanced solid tumors. Clin Cancer Res (2011) 1.61
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases. Bioorg Med Chem Lett (2007) 1.61
Hsp90-dependent activation of protein kinases is regulated by chaperone-targeted dephosphorylation of Cdc37. Mol Cell (2008) 1.57
Discovery of small molecule cancer drugs: successes, challenges and opportunities. Mol Oncol (2012) 1.55
Binding site detection and druggability index from first principles. J Med Chem (2009) 1.49
IL-1R-MyD88 signaling in keratinocyte transformation and carcinogenesis. J Exp Med (2012) 1.48
Silencing of HSP90 cochaperone AHA1 expression decreases client protein activation and increases cellular sensitivity to the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin. Cancer Res (2008) 1.48
A HIF-regulated VHL-PTP1B-Src signaling axis identifies a therapeutic target in renal cell carcinoma. Sci Transl Med (2011) 1.48
Biomarker-driven early clinical trials in oncology: a paradigm shift in drug development. Cancer J (2009) 1.46
MDpocket: open-source cavity detection and characterization on molecular dynamics trajectories. Bioinformatics (2011) 1.44
Molecular and phenotypic characterisation of paediatric glioma cell lines as models for preclinical drug development. PLoS One (2009) 1.44
High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. Anal Biochem (2004) 1.42
NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res (2008) 1.42
MGMT-independent temozolomide resistance in pediatric glioblastoma cells associated with a PI3-kinase-mediated HOX/stem cell gene signature. Cancer Res (2010) 1.40
HSP90 inhibition: two-pronged exploitation of cancer dependencies. Drug Discov Today (2011) 1.40
Objective assessment of cancer genes for drug discovery. Nat Rev Drug Discov (2013) 1.34
Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells. Cancer Res (2009) 1.34
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. J Med Chem (2009) 1.34
Potentiation of paclitaxel activity by the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin in human ovarian carcinoma cell lines with high levels of activated AKT. Mol Cancer Ther (2006) 1.33
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem Lett (2007) 1.33
Targeting Hsp90 for the treatment of cancer. Curr Opin Drug Discov Devel (2006) 1.32
A Phase II trial of 17-allylamino, 17-demethoxygeldanamycin (17-AAG, tanespimycin) in patients with metastatic melanoma. Invest New Drugs (2010) 1.30
Understanding and predicting druggability. A high-throughput method for detection of drug binding sites. J Med Chem (2010) 1.29
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res (2006) 1.29
Structure-based drug design targeting an inactive RNA conformation: exploiting the flexibility of HIV-1 TAR RNA. J Mol Biol (2004) 1.29
Magnetic resonance spectroscopic pharmacodynamic markers of the heat shock protein 90 inhibitor 17-allylamino,17-demethoxygeldanamycin (17AAG) in human colon cancer models. J Natl Cancer Inst (2003) 1.29
Inhibitors of the HSP90 molecular chaperone: attacking the master regulator in cancer. Curr Top Med Chem (2006) 1.29
EGFRvIII deletion mutations in pediatric high-grade glioma and response to targeted therapy in pediatric glioma cell lines. Clin Cancer Res (2009) 1.24
Can molecular biomarker-based patient selection in Phase I trials accelerate anticancer drug development? Drug Discov Today (2009) 1.24
Role for amplification and expression of glypican-5 in rhabdomyosarcoma. Cancer Res (2007) 1.24
Death by chaperone: HSP90, HSP70 or both? Cell Cycle (2009) 1.22
Identification of magnetic resonance detectable metabolic changes associated with inhibition of phosphoinositide 3-kinase signaling in human breast cancer cells. Mol Cancer Ther (2006) 1.21
A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera. J Mol Biol (2007) 1.20
Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther (2007) 1.19
Exploiting the cancer genome: strategies for the discovery and clinical development of targeted molecular therapeutics. Annu Rev Pharmacol Toxicol (2012) 1.19
The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway. Cancer Res (2004) 1.19
The structure of the oligopeptide-binding protein, AppA, from Bacillus subtilis in complex with a nonapeptide. J Mol Biol (2005) 1.19
In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography. Cancer Res (2006) 1.19
Inducible cutaneous inflammation reveals a protumorigenic role for keratinocyte CXCR2 in skin carcinogenesis. Cancer Res (2009) 1.17
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. Bioorg Med Chem Lett (2005) 1.17
Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone. J Med Chem (2009) 1.17
BRAF and NRAS mutations in melanoma: potential relationships to clinical response to HSP90 inhibitors. Mol Cancer Ther (2008) 1.16
Expression of kinase-defective mutants of c-Src in human metastatic colon cancer cells decreases Bcl-xL and increases oxaliplatin- and Fas-induced apoptosis. J Biol Chem (2004) 1.16
The clinical applications of heat shock protein inhibitors in cancer - present and future. Curr Cancer Drug Targets (2003) 1.16
Structure-based design of molecular cancer therapeutics. Trends Biotechnol (2009) 1.16