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DRUG:

tanespimycin (BMS-722782)

i
Other names: BMS-722782, 17-AAG, 17-allylamino-17-demethoxy-geldanamycin, KOS-953
Company:
BMS
Drug class:
HSP90 inhibitor
15d
Hsa_circ_0000520 Promotes Invasion and Metastasis of Breast Cancer Cells by Targeting HSP90AA1. (PubMed, Breast Cancer (Dove Med Press))
Rescue experiments were conducted using the HSP90AA1 inhibitor tanespimycin...Importantly, its elevated expression correlates with advanced clinical stage, specific molecular subtypes, and poor prognosis in BC patients. Our research results revealed an unrecognized regulatory axis, in which hsa_circ_0000520 facilitates BC cells progression by coordinating with HSP90AA1, highlighting hsa_circ_0000520 could be a promising diagnostic indicator and potential treatment target for BC.
Journal
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HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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tanespimycin (BMS-722782)
1m
CCNJL as a Prognostic Biomarker and Therapeutic Target in Cholangiocarcinoma. (PubMed, Curr Med Chem)
CCNJL has the potential to act as a valuable prognostic indicator and immunotherapy target in CHOL. Its expression pattern and associations with clinical outcomes, immune characteristics, and drug sensitivity highlight its potential for improving diagnostic and therapeutic approaches. Future research should focus on elucidating the underlying mechanisms and validating these findings in larger cohorts.
Journal • IO biomarker
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CD8 (cluster of differentiation 8)
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Koselugo (selumetinib) • tanespimycin (BMS-722782) • elesclomol (STA-4783)
2ms
Integrating Network Toxicology, Machine Learning, and Experimental Evidence Reveals Candidate Targets and Pathways in PCDD/F-Related Colon Cancer. (PubMed, Food Chem Toxicol)
Consistent with these in silico findings, exposure of mice to 24 μg/kg TCDF significantly increased the expression of Mmp7 and Hsp90aa1 in murine colonic tissues, increased the levels of proinflammatory cytokines Ifn-γ, Il-1β, and Il-6, and downregulated the expression of Mucin 2 (MUC2). Connectivity Map analysis based on the PCDD/F-related gene signature identified five candidate compounds targeting MMP7 and HSP90AA1, of which four HSP90 inhibitors (tanespimycin, alvespimycin, NVP-AUY922 and AT-13387) showed negative connectivity scores, suggesting potential to reverse the pollutant-induced expression profile.
Journal
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IFNG (Interferon, gamma) • IL6 (Interleukin 6) • IL1B (Interleukin 1, beta) • MUC2 (Mucin 2) • MMP7 (Matrix metallopeptidase 7)
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tanespimycin (BMS-722782) • luminespib (AUY922) • onalespib (AT13387)
5ms
A High-Density Microchamber Array for the Analysis of Extracellular Vesicles Derived from Single Cells under Drug Treatment. (PubMed, Anal Chem)
Here, we study EV secretion from individual breast cancer cells and the changes under treatment with the HSP90-inhibiting cancer drug tanespimycin (17AAG)...Moreover, our results emphasize that using CD63 as the sole EV capture protein may hide important EV subpopulations. Overall, our platform may support future choices of EV biomarkers for diagnostic and biomedical purposes and help in understanding the heterogeneous drug response of cancer cells.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • CD9 (CD9 Molecule) • CD81 (CD81 Molecule) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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HER-2 positive
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tanespimycin (BMS-722782)
7ms
Andrographolide Promotes Ferroptosis in Pancreatic Cancer via Targeting and Activating HSP90/GPX4 Ubiquitination. (PubMed, Biofactors)
ADG suppresses HSP90 expression, and tanespimycin prevents ADG-induced cytotoxicity, showing that HSP90 is ADG's main target in activating intracellular activities...The findings strongly suggest that ADG may treat PC. ADG's pharmacokinetics and other effects must be studied in patients' clinical trials to make it a pancreatic cancer therapy option.
Journal • IO biomarker
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GPX4 (Glutathione Peroxidase 4) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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tanespimycin (BMS-722782)
7ms
Identification of key genes in pancreatic ductal adenocarcinoma with biologically informed deep neural network. (PubMed, J Gastrointest Oncol)
Through molecular docking analysis, we found that ursolic acid (UA) and tanespimycin might target JAG1, MET, and PLAU...Our study demonstrated that JAG1, MET, and PLAU were significantly overexpressed and associated with poor outcomes in PDAC patients. More importantly, these genes are involved in the crosstalk between tumour and immune cells, which indicates that these genes may serve as novel targets for combination immunotherapy in the treatment of PDAC.
Journal • IO biomarker
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JAG1 (Jagged Canonical Notch Ligand 1) • PLAU (Plasminogen Activator)
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tanespimycin (BMS-722782)
11ms
Tick-Tock: Cancer Cell Division Cycle Clocks Strike Midnight. (PubMed, Int J Mol Sci)
To induce these potential forced overgrowth effects, we suggest targeting the cell division cycle regulatory enzyme, the anaphase-promoting complex/cyclosome (APC/C), to suppress-but not inhibit-its activity. We conclude by proposing experiments to test this hypothesis in which an APC/C inhibitor, such as a low level of proTAME, is combined with the clinically approved heat-shock protein 90 (HSP90)-inhibitor pimitespib (TAS-116) or the pre-clinical molecule tanespimycin, which, to the best of our knowledge, are combinations that have not been investigated before.
Review • Journal
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HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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tanespimycin (BMS-722782) • Jeselhy (pimitespib)
1year
Pd, S co-modified Prussian blue analogues nanocomposites for MRI guided combined mitochondria-targeting cancer therapy with tumor microenvironment remodeling, multienzyme-like catalysis and mild photothermal therapeutic effect. (PubMed, Colloids Surf B Biointerfaces)
To construct efficient nanoplatform for prostate cancer therapy, a HSP 90 protein inhibitor, tanespimycin was loaded on Pd-S-CNMF (17Pd-S-CNMF) to inhibit the level of HSP 90 protein, thus increasing the outcome of subsequent photothermal therapy...Benefiting from these amazing properties, the as-prepared 17Pd-S-CNMF could effectively inhibit the growth of prostate cancer in vitro and vivo. Our findings provide a paradigm for construction of efficient nanocomposites as nanoplatform for cancer diagnose and treatment.
Journal
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HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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tanespimycin (BMS-722782)
over1year
Consensus nonnegative matrix factorization reveals metastatic gene expression program and identifies E74-like ETS transcription factor 3 confers to the lymph nodes metastasis in papillary thyroid cancer. (PubMed, Endocrine)
This study highlights the critical role of GEP and ELF3 in driving PTC progression and metastasis. Drug screening revealed that tanespimycin and vemurafenib were effective in targeting GEP3high cells, offering therapeutic potential for aggressive PTC. These insights advance precision strategies for managing metastatic and heterogeneous PTC by targeting ELF3-driven pathways.
Journal
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BRAF (B-raf proto-oncogene) • TCF3 (Transcription Factor 3) • ELF3 (E74 Like ETS Transcription Factor 3)
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BRAF V600E
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Zelboraf (vemurafenib) • tanespimycin (BMS-722782)
over1year
An in vitro pharmacogenomic approach reveals subtype-specific therapeutic vulnerabilities in atypical teratoid/rhabdoid tumors (AT/RT). (PubMed, Pharmacol Res)
Subtype-dependent drug response profiles demonstrated sensitivity of AT/RT-SHH cell lines to B-cell lymphoma 2 (BCL2) and heat shock protein 90 (HSP90) inhibitors, and increased activity of microtubule inhibitors, kinesin spindle protein (KSP) inhibitors, and the eukaryotic translation initiation factor 4E (eIF4E) inhibitor briciclib in a subset of AT/RT-MYC cell lines. In summary, our in vitro pharmacogenomic approach revealed preclinical evidence of tumor type- and subtype-specific therapeutic vulnerabilities in AT/RT cell lines that may inform future in vivo and clinical evaluations of novel pharmacological strategies.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • SMARCA4 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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Venclexta (venetoclax) • idasanutlin (RG7388) • tanespimycin (BMS-722782) • ABT-737 • briciclib (ON 013105) • GDC-0623
over1year
ZP3 Expression in Pancreatic Adenocarcinoma: Its Implications for the Prognosis and Therapy. (PubMed, Protein Pept Lett)
ZP3 has the potential to serve as a prognostic biomarker and therapeutic target for patients with PAAD.
Journal • Tumor mutational burden
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TMB (Tumor Mutational Burden) • MSI (Microsatellite instability)
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docetaxel • Koselugo (selumetinib) • tanespimycin (BMS-722782) • bleomycin
over1year
Thermo-Responsive Gold Nanorod Vesicles for Combined NIR-II Photothermal Therapy and Chemotherapy of Solid Tumors. (PubMed, Acta Biomater)
Upon 1064 nm laser irradiation, USGRV-17-AAG exhibits a high photothermal conversion efficiency (65.1%) and thus can achieve temperature responsive release of tanespimycin (17-AAG), an inhibitor of HSP90...Additionally, USGRV-17-AAG exhibited efficient photothermal conversion (65.1%) under 1064 nm laser irradiation and enabled temperature-responsive drug release through the action of surface-modified upper critical solution temperature (UCST) polymers. This nanocarrier, with enhanced NIR-II photothermal therapy, might offer a promising solution for anti-tumor treatment.
Journal
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AVEN (Apoptosis And Caspase Activation Inhibitor) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
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tanespimycin (BMS-722782)