A fluorescence polarization assay for inhibitors of Hsp90

The Protein Data Bank

2000 • 35,287 citations

PROCHECK: a program to check the stereochemical quality of protein structures

1993 • 23,689 citations

The CCP4 suite: programs for protein crystallography

1994 • 17,203 citations

Refinement of Macromolecular Structures by the Maximum-Likelihood Method

1997 • 14,729 citations

Improved methods for building protein models in electron density maps and the location of errors in these models

1991 • 12,831 citations

Automated protein model building combined with iterative structure refinement.

1999 • 2,428 citations

Regulation of Signaling Protein Function and Trafficking by the hsp90/hsp70-Based Chaperone Machinery

2003 • 1,470 citations

Crystal Structure of an Hsp90–Geldanamycin Complex: Targeting of a Protein Chaperone by an Antitumor Agent

1997 • 1,345 citations

The 90-kDa Molecular Chaperone Family

1998 • 1,008 citations

Structural Basis for Inhibition of the Hsp90 Molecular Chaperone by the Antitumor Antibiotics Radicicol and Geldanamycin

1999 • 979 citations

Modulation of Akt kinase activity by binding to Hsp90

2000 • 942 citations

Macromolecular Crystallography Part A

1997 • 779 citations

Hsp90 & Co. – a holding for folding

1999 • 631 citations

Implementation of molecular replacement in AMoRe

2001 • 621 citations

Heat shock protein 90 as a molecular target for cancer therapeutics

2003 • 572 citations

HSP90 as a new therapeutic target for cancer therapy: the story unfolds

2002 • 526 citations

Activation of the ATPase Activity of Hsp90 by the Stress-Regulated Cochaperone Aha1

2002 • 515 citations

Preclinical pharmacologic evaluation of geldanamycin as an antitumor agent

1995 • 496 citations

Disruption of the Raf-1-Hsp90 Molecular Complex Results in Destabilization of Raf-1 and Loss of Raf-1-Ras Association

1995 • 454 citations

Antibiotic radicicol binds to the N-terminal domain of Hsp90 and shares important biologic activities with geldanamycin

1998 • 396 citations

Structure and in vivo function of Hsp90

2000 • 317 citations

Fluorescence Polarization and Anisotropy in High Throughput Screening: Perspectives and Primer

2000 • 289 citations

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

2001 • 282 citations

Structural basis for recruitment of the ATPase activator Aha1 to the Hsp90 chaperone machinery

2004 • 282 citations

Inhibition of signal transduction by the Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin results in cytostasis and apoptosis.

2001 • 281 citations

Structure-Activity Relationships in Purine-Based Inhibitor Binding to HSP90 Isoforms

2004 • 255 citations

Aha1 Binds to the Middle Domain of Hsp90, Contributes to Client Protein Activation, and Stimulates the ATPase Activity of the Molecular Chaperone

2003 • 215 citations

Altered states: selectively drugging the Hsp90 cancer chaperone

2004 • 205 citations

Development of High Throughput Screening Assays Using Fluorescence Polarization: Nuclear Receptor-Ligand–Binding and Kinase /Phosphatase Assays

2000 • 202 citations

Structure, function, and mechanism of the Hsp90 molecular chaperone

2001 • 199 citations

Homogeneous fluorescence readouts for miniaturized high-throughput screening: theory and practice

1999 • 195 citations

Development of a Purine-Scaffold Novel Class of Hsp90 Binders that Inhibit the Proliferation of Cancer Cells and Induce the Degradation of Her2 Tyrosine Kinase

2002 • 193 citations

High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity

2004 • 190 citations

Crystal Structure and Molecular Modeling of 17-DMAG in Complex with Human Hsp90

2003 • 189 citations

17AAG: low target binding affinity and potent cell activity--finding an explanation.

2003 • 151 citations

Inhibition of Hsp90: a new strategy for inhibiting protein kinases

2003 • 146 citations

Metabolism of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) by murine and human hepatic preparations.

1998 • 132 citations

Halohydrin and Oxime Derivatives of Radicicol: Synthesis and Antitumor Activities

2002 • 109 citations

Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics.

2003 • 108 citations

Development of Purine-Scaffold Small Molecule Inhibitors of Hsp90

2003 • 104 citations

Identification of SSF1, CNS1, and HCH1 as multicopy suppressors of a Saccharomyces cerevisiae Hsp90 loss-of-function mutation

1999 • 100 citations

Development of a Fluorescence Polarization Assay for the Molecular Chaperone Hsp90

2004 • 89 citations

Hsp90, not Grp94, regulates the intracellular trafficking and stability of nascent ErbB2

2002 • 78 citations

Radicicol-sensitive Peptide Binding to the N-terminal Portion of GRP94

2002 • 74 citations

Heat shock protein 90 inhibition by 17-allylamino-17- demethoxygeldanamycin: a novel therapeutic approach for treating hormone-refractory prostate cancer.

2002 • 66 citations

Adenine derived inhibitors of the molecular chaperone HSP90—SAR explained through multiple X-ray structures

2003 • 62 citations

A time-resolved fluorescence resonance energy transfer-based HTS assay and a surface plasmon resonance-based binding assay for heat shock protein 90 inhibitors

2004 • 52 citations

Synthesis and Antitumor Activity of Novel O-Carbamoylmethyloxime Derivatives of Radicicol

2003 • 46 citations

Fluorescence Polarization Standards for High-Throughput Screening and Imaging

2002 • 35 citations

Single-Molecule Detection Technologies in Miniaturized High-Throughput Screening: Fluorescence Intensity Distribution Analysis

2003 • 35 citations

Geldanamycin-induced cytotoxicity in human colon-cancer cell lines: evidence against the involvement of c-Src or DT-diaphorase

1998 • 28 citations

Filter binding assay for the geldanamycin–heat shock protein 90 interaction

2003 • 26 citations

Assays for HSP90 and Inhibitors

2003 • 25 citations