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NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.
The data show that NVP-AUY922 is a potent, novel inhibitor of HSP90, acting via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis. Expand
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
- P. Brough, W. Aherne, +34 authors L. Wright
- Chemistry, Medicine
- Journal of medicinal chemistry
- 20 November 2007
The structure-based design, synthesis, structure-activity relationships and pharmacokinetics of potent small-molecule inhibitors of Hsp90 based on the 4,5-diarylisoxazole scaffold are described and analogues from this series have high affinity for HSp90, as measured in a fluorescence polarization (FP) competitive binding assay, and are active in cancer cell lines. Expand
DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90.
- L. Kèlland, S. Sharp, P. Rogers, T. Myers, P. Workman
- Biology, Medicine
- Journal of the National Cancer Institute
- 17 November 1999
The results suggest that the antitumor activity and possibly the toxicologic properties of 17AAG in humans may be influenced by the expression of DT-diaphorase. Expand
Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells.
Low NQO1 activity is a likely mechanism of acquired resistance to 17-AAG in GB, melanoma, and, possibly, other tumor types and can be overcome with novel HSP90 inhibitors. Expand
Inhibitors of the HSP90 molecular chaperone: current status.
It is not surprising that new HSP90 agents are under development against this novel target for cancer therapy and several show promise, but there are several limitations with 17-AAG such as solubility, stability, and hepatotoxicity. Expand
MGMT-independent temozolomide resistance in pediatric glioblastoma cells associated with a PI3-kinase-mediated HOX/stem cell gene signature.
An in vitro link between phosphoinositide 3-kinase-mediated HOXA9/HOXA10 expression, and a drug-resistant, progenitor cell phenotype in MGMT-independent pediatric glioblastoma is shown. Expand
Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells.
The findings indicate that the effects of HSP90 inhibition on mRNA splicing may prove beneficial in prostate cancers expressing AR-V7, supporting further clinical investigation of H SP90 inhibitors in malignancies no longer responsive to androgen deprivation. Expand
EGFRvIII Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines
- D. Bax, N. Gaspar, +16 authors Chris Jones
- Medicine, Biology
- Clinical Cancer Research
- 15 September 2009
These data identify an elevated frequency of EGFR gene amplification and EGFRvIII mutation in pediatric HGG than previously recognized and show the likely necessity of targeting multiple genetic alterations in the tumors of these children. Expand
Heat shock protein inhibition is associated with activation of the unfolded protein response pathway in myeloma plasma cells.
Hsp90 inhibitors induce myeloma cell death at least in part via endoplasmic reticulum stress and the UPR death pathway. Expand
Silencing of HSP90 cochaperone AHA1 expression decreases client protein activation and increases cellular sensitivity to the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin.
AHA1 (activator of HSP90 ATPase) is a cochaperone of the ATP-dependent molecular chaperone, HSP90, which is involved in the maturation, stabilization/degradation, and function of oncogenic proteins.… Expand