Gabriela Chiosis

Synthesis of a red-shifted fluorescence polarization probe for Hsp90.

Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function.

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.

BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90.

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

Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol.

Vancomycin resistance: occurrence, mechanisms and strategies to combat it.

Microtiter cell-based assay for detection of agents that alter cellular levels of Her2 and EGFR.

Development of purine-scaffold small molecule inhibitors of Hsp90.

Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.

General method for the synthesis of 8-arylsulfanyl adenine derivatives.

Targeting wide-range oncogenic transformation via PU24FCl, a specific inhibitor of tumor Hsp90.

Development of a fluorescence polarization assay for the molecular chaperone Hsp90.

Hsp90: the vulnerable chaperone.

Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.

Small molecule microarrays: from proteins to mammalian cells - are we there yet?

Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90.

Targeting chaperones in transformed systems--a focus on Hsp90 and cancer.

New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies.

Synthesis of Hsp90 dimerization modulators.

Identification of novel quaternary domain interactions in the Hsp90 chaperone, GRP94.

Heat shock protein-90 inhibitors: a chronicle from geldanamycin to today's agents.

Discovery and development of purine-scaffold Hsp90 inhibitors.

Hsp70 molecular chaperones: emerging roles in human disease and identification of small molecule modulators.

Structural and quantum chemical studies of 8-aryl-sulfanyl adenine class Hsp90 inhibitors.

Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators.

Purine-scaffold Hsp90 inhibitors.

Tumor selectivity of Hsp90 inhibitors: the explanation remains elusive.

Roles of heat-shock protein 90 in maintaining and facilitating the neurodegenerative phenotype in tauopathies.

Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.

High-throughput screening fluorescence polarization assay for tumor-specific Hsp90.

Anti-cancer therapeutic approaches based on intracellular and extracellular heat shock proteins.

Molecular imaging of the efficacy of heat shock protein 90 inhibitors in living subjects.

Development and application of Hsp90 inhibitors.

The chaperone activity of heat shock protein 90 is critical for maintaining the stability of leucine-rich repeat kinase 2.

Design of a fluorescence polarization assay platform for the study of human Hsp70.

The yeast Hsp110, Sse1p, exhibits high-affinity peptide binding.

Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.

Targeting Hsp90: small-molecule inhibitors and their clinical development.

Kaiso contributes to DNA methylation-dependent silencing of tumor suppressor genes in colon cancer cell lines.

Discovery and development of heat shock protein 90 inhibitors.

Microwave-assisted one step synthesis of 8-arylmethyl-9H-purin-6-amines.

Heat shock protein 90: translation from cancer to Alzheimer's disease treatment?

Assay for isolation of inhibitors of her2-kinase expression.

Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models.

Targeting heat shock protein 90 with non-quinone inhibitors: a novel chemotherapeutic approach in human hepatocellular carcinoma.

Purine-scaffold Hsp90 inhibitors.

A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6-dependent B cell lymphomas.

Measuring the pharmacodynamic effects of a novel Hsp90 inhibitor on HER2/neu expression in mice using Zr-DFO-trastuzumab.

Synthesis of reblastatin, autolytimycin, and non-benzoquinone analogues: potent inhibitors of heat shock protein 90.

Heat shock protein 90 in neurodegenerative diseases.

Assay strategies for the discovery and validation of therapeutics targeting Brugia pahangi Hsp90.

HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans.

The anti-myeloma activity of a novel purine scaffold HSP90 inhibitor PU-H71 is via inhibition of both HSP90A and HSP90B1.

BCL6 repression of EP300 in human diffuse large B cell lymphoma cells provides a basis for rational combinatorial therapy.

Design of a flexible cell-based assay for the evaluation of heat shock protein 70 expression modulators.

Heat shock protein 90-sheltered overexpression of insulin-like growth factor 1 receptor contributes to malignancy of thymic epithelial tumors.

Design, synthesis, and evaluation of small molecule Hsp90 probes.

Synthesis of purine-scaffold fluorescent probes for heat shock protein 90 with use in flow cytometry and fluorescence microscopy.

Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90.

HSP90 inhibitors as therapy for multiple myeloma.

Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers.

Advances in the discovery and development of heat-shock protein 90 inhibitors for cancer treatment.

Targeting of KRAS mutant tumors by HSP90 inhibitors involves degradation of STK33.

Heat shock protein gp96 regulates Toll-like receptor 9 proteolytic processing and conformational stability.

Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy.

Discovery and validation of small-molecule heat-shock protein 90 inhibitors through multimodality molecular imaging in living subjects.

The novel HSP90 inhibitor, PU-H71, suppresses glial cell activation but weakly affects clinical signs of EAE.

A global view of Hsp90 functions.

Discovery and development of purine-scaffold Hsp90 inhibitors.

Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.

Synthesis and evaluation of cell-permeable biotinylated PU-H71 derivatives as tumor Hsp90 probes.

α7 helix region of αI domain is crucial for integrin binding to endoplasmic reticulum chaperone gp96: a potential therapeutic target for cancer metastasis.

Posttranslational modification and conformational state of heat shock protein 90 differentially affect binding of chemically diverse small molecule inhibitors.

Targeting the Hsp90-associated viral oncoproteome in gammaherpesvirus-associated malignancies.

Experimental and Structural Testing Module to Analyze Paralogue-Specificity and Affinity in the Hsp90 Inhibitors Series.

Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2.

Molecular chaperone gp96 is a novel therapeutic target of multiple myeloma.

A purine analog synergizes with chloroquine (CQ) by targeting Plasmodium falciparum Hsp90 (PfHsp90).

Identification of an allosteric pocket on human hsp70 reveals a mode of inhibition of this therapeutically important protein.

Regulatory chaperone complexes in neurodegenerative diseases: a perspective on therapeutic intervention.

Pre-clinical efficacy of PU-H71, a novel HSP90 inhibitor, alone and in combination with bortezomib in Ewing sarcoma.

Improved targeting of JAK2 leads to increased therapeutic efficacy in myeloproliferative neoplasms.

Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70.

Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70.

Environment-responsive nanophores for therapy and treatment monitoring via molecular MRI quenching.

Heat shock protein 90 inhibitors in the treatment of cancer: current status and future directions.

Protein chaperones: a composition of matter review (2008 - 2013).

Affinity purification probes of potential use to investigate the endogenous Hsp70 interactome in cancer.

Chaperone-dependent Neurodegeneration: A Molecular Perspective on Therapeutic Intervention.