Hsp90 inhibitor
HSP90 inhibitor geldanamycin reverts IL 13– and IL 17–induced airway goblet cell metaplasia
... HDAC6 inhibitor ISOX caused a dramatic reduc- tion in the total number of cells and an increase in nonciliated/ nongoblet cells with decreased epithelial thickness (Figure 5, A, D, and E) at the dose ...the ...
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First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors.
... Durable target inhibition and antitumor activity was seen with weekly administered HSP90 inhibitors in a human NSCLC xenograft mouse model (25, 26). However, suppression of the client proteins in humans could be ...
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<p>Antitumorigenic Effect of Hsp90 Inhibitor SNX-2112 on Tongue Squamous Cell Carcinoma is Enhanced by Low-Intensity Ultrasound</p>
... the Hsp90 inhibitor, 17AAG, modulated unfold protein response and sensitized prostate cancer to ...decrease Hsp90 expression (Figures 4C and 5C), and increased the expression of PERK, CHOP and BAX, ...
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Radiosensitization of HSF-1 Knockdown Lung Cancer Cells by Low Concentrations of Hsp90 Inhibitor NVP-AUY922
... most Hsp90 inhibitors activate HSF-1 that induces the transcription of cytoprotective and tumor- promoting stress proteins such as Hsp70 and Hsp27, a combined approach consisting of HSF-1 knockdown ...and ...
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Sensitization of Chemo-Resistant Human Chronic Myeloid Leukemia Stem-Like Cells to Hsp90 Inhibitor by SIRT1 Inhibition
... hibiting Hsp90 have been shown to possess multiple intracellular targeting capacities and could potentially be active against many types of cancer through deg- radation of a large number of client proteins ...that ...
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Ribosome Profiling Reveals HSP90 Inhibitor Effects on Stage-Specific Protein Synthesis in Leishmania donovani
... by HSP90 inhibition of L. donovani parasites. HSP90 activity or the lack thereof affects the synthesis of several chaperone proteins, but also of histones, amastins, proteolytic proteins, and redox ...the ...
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HSP90 inhibitor AUY922 induces cell death by disruption of the Bcr-Abl, Jak2 and HSP90 signaling network complex in leukemia cells
... of HSP90 are produced leading to the formation of the large network ...of HSP90 and its client proteins in Bcr-Abl+ cells ...of HSP90 activity by the specific HSP90 inhibitor would ...
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Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX
... to HSP90 inhibitors is possible and their ability to induce apoptosis is less than might be ...the HSP90 inhibitor 17-AAG both in vitro and in tumor xenografts in ...
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Reactivation of ERK and Akt confers resistance of mutant BRAF colon cancer cells to the HSP90 inhibitor AUY922
... (HSP90) inhibitor AUY922, and that this is caused by rebound activation of ERK and ...of HSP90, was only partially degraded by AUY922, whereas reactivation of Akt was related to the activity of the ...
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NVP-AUY922, a novel HSP90 inhibitor, inhibits the progression of malignant pheochromocytoma in vitro and in vivo
... The HSP90 inhibitor, NVP-AUY922, and 17-AAG were purchased from Selleck Chemicals (Houston, TX, USA) and solubilized in dimethyl sulfoxide (DMSO) to a concentration of 1 mM/mL before ...
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Hsp90 inhibitor 17-allylamino-17-demethoxygeldanamycin inhibits the proliferation of ARPE-19 cells
... of Hsp90 (heat shock protein 90), is currently under- going phase II/III clinical trials as the first Hsp90 inhibitor to treat ...tumors. Hsp90 is a chaperone protein that participates in the ...
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HSP90 Inhibitor Encapsulated Photo-Theranostic Nanoparticles for Synergistic Combination Cancer Therapy
... (Hsp90) inhibitor simultaneously for combination therapy against prostate ...of Hsp90 inhibitors that can decrease the levels of pro-survival and angiogenic signaling molecules induced by ...
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NVP AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models
... Since NVP-AUY922 exhibited a strong antiproliferative effect against established and primary breast cancer cells (Tables 1 and 2), we evaluated the properties of the compound in vivo. To this end, a breast cancer ...
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Hsp90 inhibitor NMS-E973 exerts the anticancer effect against glioblastoma via induction of PUMA-mediated apoptosis
... In conclusion, our study demonstrates a potential thera- peutic strategy of using NMS-E973 against glioblastoma by proving the antitumor mechanism of action of NMS-E973 via PUMA-mediated apoptosis. These findings are in ...
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Molecular signature of response and potential pathways related to resistance to the HSP90 inhibitor, 17AAG, in breast cancer
... 17AAG occurring in resistant cells, to define genes or pathways commonly involved in insensitivity to this drug. The identification of pathways in relation to 17AAG resistance would be important to develop in future ...
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Effects of 17 allylamino 17 demethoxygeldanamycin (17 AAG) in transgenic mouse models of frontotemporal lobar degeneration and Alzheimer’s disease
... a Hsp90 client protein. Hsp90 assists protein folding and stabilization of its client protein, and 17-AAG is an Hsp90 ...though Hsp90 co-localized in vivo with amyloid filaments, indicating ...
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Spotlight on the microbes that produce heat shock protein 90-targeting antibiotics
... 13 Hsp90 inhibitor compounds now being in phase I/II clinical trials for the treatment of various cancers ...sustained Hsp90 chaperone activity, but the Hsp90 in cancer cells has a higher ...
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HSP90 Protects the Human T-Cell Leukemia Virus Type 1 (HTLV-1) Tax Oncoprotein from Proteasomal Degradation To Support NF-κB Activation and HTLV-1 Replication
... between HSP90 and Tax was validated by coimmunoprecipitation assays, and colo- calization between the two proteins was observed by confocal ...the HSP90 inhibitor 17-DMAG elicited proteasomal ...
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Inhibition of heat shock protein 90 improves pulmonary arteriole remodeling in pulmonary arterial hypertension
... a HSP90 inhibitors as therapeutic drugs for PAH treatment, might affect other pathological and physiological processes, such as oxidative stress or neoangiogenesis [14, ...of HSP90 inhibitor as a ...
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Docking of Human Heat Shock Protein 90 with Selenoderivatives of Geldanamycin
... in HSP90 inhibitor ...to HSP90 stronger than GMD, while maintaining lipophilic interactions and hydrogen bonds with amino acid residues like Asp93, which are catalytically crucial for therapeutic ...
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