tanespimycin (BMS-722782) / BMS 
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  • ||||||||||  Jakafi (ruxolitinib) / Incyte, ganetespib (ADX-1612) / Aldeyra, tanespimycin (BMS-722782) / BMS
    Heat shock protein inhibitors suppress cytokine-induced DUOX2 mRNA and protein expression in human pancreatic cancer cells in a JAK-STAT dependent manner [WITHDRAWN] (Section 11; Poster Board No: 11) -  Mar 25, 2025 - Abstract #AACR2025AACR_4634;    
    Using a panel of human pancreatic cancer cell lines (BxPC-3, AsPC-1 and CFPAC-1), we found that two different Hsp90 inhibitors, Tanespimycin (17-AAG) and Ganetespib (STA-9090), inhibit JAK1 and JAK2 kinases, blocking cytokine-induced, JAK-regulated STAT phosphorylation...Furthermore, the JAK1/2 inhibitor Ruxolitinib inhibits IL-4 induced and JAK-mediated STAT6 phosphorylation, and DUOX2 mRNA and protein expression in BxPC-3 cells...Either remaining Hsp90 protein or other isoforms of Hsp90 in cells may compensate decreased Hsp90 function after siRNA knockdown. Our data suggests that Hsp90 inhibitors, through blocking the cytokine-activated JAK-STATs oncogenic signaling pathway and their downstream genes such as DUOX2, VEGF-A, MMP-7 and PD-L1expression, may be a valuable therapeutic approach for inflammation-associated pancreatic cancer.
  • ||||||||||  tanespimycin (BMS-722782) / BMS, Tudcabil (tauroursodeoxycholic acid) / Bruschettini
    Review, Journal:  Pharmacological landscape of endoplasmic reticulum stress: uncovering therapeutic avenues for metabolic diseases. (Pubmed Central) -  Mar 16, 2025   
    The review emphasizes challenges in translating these therapies to clinical applications, such as toxicity, off-target effects, limited bioavailability, and the lack of large-scale randomized controlled trials (RCTs). It also highlights the potential of personalized medicine approaches and pharmacogenomics in optimizing ER stress-targeting therapies.
  • ||||||||||  Preclinical, Journal, IO biomarker:  An in vitro pharmacogenomic approach reveals subtype-specific therapeutic vulnerabilities in atypical teratoid/rhabdoid tumors (AT/RT). (Pubmed Central) -  Mar 9, 2025   
    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.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Thermo-Responsive Gold Nanorod Vesicles for Combined NIR-II Photothermal Therapy and Chemotherapy of Solid Tumors. (Pubmed Central) -  Jan 15, 2025   
    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.
  • ||||||||||  tanespimycin (BMS-722782) / BMS, dinaciclib (MK-7965) / Merck (MSD), AZD4573 / AstraZeneca
    Preclinical, Journal:  Mechanisms and efficacy of small molecule "latency promoting agents" to inhibit HIV reactivation ex vivo. (Pubmed Central) -  Aug 20, 2024   
    By selecting drugs with known mechanisms of action, we specifically identified cellular factors and pathways that may be involved in regulation of HIV expression. These drugs/targets deserve further study in strategies aimed at reducing HIV-associated immune activation or achieving a functional cure.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Mechanistic study of pre-eclampsia and macrophage-associated molecular networks: bioinformatics insights from multiple datasets. (Pubmed Central) -  Jun 7, 2024   
    We propose that these genes play a crucial role in regulating the maternal-fetal immune microenvironment in PE patients, and the pathways associated with these genes offer potential avenues for exploring the molecular mechanisms underlying preeclampsia and identifying therapeutic targets. Additionally, by utilizing the Connectivity Map database, we identified drug targets like Ttnpb, Doxorubicin, Tyrphostin AG 825, and Tanespimycin as potential clinical treatments for preeclampsia.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Synthetic optimization and biological characterization of phenylethynesulfonamide derivatives | Poster Board #936 (In-person; Poster Board #936; Hall C (Ernest N. Morial Convention Center)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_12666;    
    The heat shock protein 90 inhibitor, tanespimycin, was used as a positive control. Tanespimycin displayed increasing heat shock promoter induction with longer time frames, while the PES derivatives induced the heat shock promoter element equally after treatment times between 5 and 18 hours.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Peptomer linkers for controlled release of small molecule chemotherapeutics (Hybrid; Gravier C Ballroom (New Orleans Marriott Warehouse Arts District)) -  Mar 12, 2024 - Abstract #ACSSp2024ACS_Sp_8822;    
    We next selected our fastest and slowest-degrading peptomers and conjugated them to different therapeutics (doxorubicin and tanespimycin) to demonstrate multi-stage release. These results indicate the potential of peptomer drug linkers to address current limitations in combination chemotherapeutic delivery and provide a route to tune release kinetics for differential dosing schedules of more than one active agent.
  • ||||||||||  Journal:  Inhibition of HSP90 distinctively modulates the global phosphoproteome of Leishmania mexicana developmental stages. (Pubmed Central) -  Dec 17, 2023   
    We measured changes in phosphorylation of many RBPs and signaling proteins including protein kinases upon HSP90 inhibition in the therapeutically relevant amastigote stage. This work provides insights into the importance of HSP90-mediated protein cross-talks and regulation of phosphorylation in Leishmania, thus significantly expanding our knowledge of the posttranslational modification in Leishmania biology.
  • ||||||||||  zelavespib intravenous (PU-H71 IV) / Samus Therap, tanespimycin (BMS-722782) / BMS
    Journal:  Co-targeting HSP90 alpha and CDK7 overcomes resistance against HSP90 inhibitors in BCR-ABL1+ leukemia cells. (Pubmed Central) -  Dec 11, 2023   
    Remarkably, combined CDK7 and HSP90 inhibition display synergistic activity against therapy-resistant BCR-ABL1+ patient leukemia cells via blocking pro-survival HSR and HSP90? overexpression, providing a novel strategy to avoid the emergence of resistance against treatment with HSP90i alone.
  • ||||||||||  trichostatin A (VTR-297) / Vanda, LY294002 / Eli Lilly, tanespimycin (BMS-722782) / BMS
    Journal:  Idiopathic Pulmonary Arterial Hypertension: Network-Based Integration of Multi-Omics Data Reveals New Molecular Signatures and Candidate Drugs. (Pubmed Central) -  Jul 21, 2023   
    In addition, the salient gene-based drug repositioning analysis identified alvespimycin, tanespimycin, geldanamycin, LY294002, cephaeline, digoxigenin, lanatoside C, helveticoside, trichostatin A, phenoxybenzamine, genistein, pioglitazone, and rosiglitazone as potential drug candidates for IPAH. In conclusion, this study provides new molecular signatures in relation to IPAH and attendant potential drug candidates for further experimental and translational clinical research for patients with IPAH.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Preclinical, Journal:  The role of heat shock protein 90 in the proliferation of Babesia gibsoni in vitro. (Pubmed Central) -  Jul 17, 2023   
    Moreover, two HSP90 inhibitors, geldanamycin (GA) and tanespimycin (17-AAG), were used to evaluate the function of BgHSP90...This result indicated that GA inhibited the function of canine neutrophils. Additional studies are necessary to elucidate the role of BgHSP90 in the proliferation of the parasite.
  • ||||||||||  Synribo (omacetaxine mepesuccinate) / Stragen, Teva, tanespimycin (BMS-722782) / BMS
    Journal:  Elucidating host cell response pathways and repurposing therapeutics for SARS-CoV-2 and other coronaviruses. (Pubmed Central) -  Nov 14, 2022   
    In-depth analysis highlighted proteasome, ribosome, and heat shock pathways as key targets in modulating host responses during viral infection. Further studies of these pathways and compounds have provided novel and impactful insights into SARS-CoV-2 biology and host responses that could be further leveraged for COVID-19 therapeutics development.
  • ||||||||||  Zolinza (vorinostat) / Merck (MSD), tanespimycin (BMS-722782) / BMS
    Journal:  Exploring the oncogenic and therapeutic target potential of the MYB-TYK2 fusion gene in B-cell acute lymphoblastic leukemia. (Pubmed Central) -  Aug 26, 2022   
    Importantly, these findings indicate that activating TYK2 alterations can function as driver oncogenes rather than passenger or secondary events in disease development. In addition, our data provide evidence for use of vorinostat and cerdulatinib in the treatment regimens of patients with this rare yet aggressive type of high-risk ALL that warrants further investigation in the clinical setting.
  • ||||||||||  amantadine / Generic mfg.
    Journal:  Multistage signal-interactive nanoparticles improve tumor targeting through efficient nanoparticle-cell communications. (Pubmed Central) -  Feb 11, 2022   
    This biochemical transceiver can act as both the signal receiver for amantadine to achieve NP transformation and signal conversion as well as the signal source to present different signals sequentially by reversible self-mimicking. Compared with the non-interactive controls, these signal-interactive NPs loaded with AS1411 and tanespimycin (17-AAG) as anticancer drugs improve tumor targeting 2.8-fold and tumor suppression 6.5-fold and showed only 51% accumulation in the liver with restricted hepatic injury.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Nanocarrier-mediated immunogenic chemotherapy for triple negative breast cancer. (Pubmed Central) -  Jun 22, 2021   
    To remodel the tumor microenvironment, we developed a liposome formulation to deliver a potential immunogenic cell death (ICD) inducing agent, 17-(allylamino)-17-demethoxygeldanamycin (17-AAG, or tanespimycin), in a tumor targeted manner to reverse the immunosuppressive microenvironment and facilitate the checkpoint blockade immunotherapy...Despite the fact that low dose 17-AAG liposomes demonstrated a limited therapeutic effect alone on 4 T1 tumor, promising efficacy was observed when 17-AAG liposomes combined with checkpoint blockade immunotherapy. Taken together, 17-AAG liposomes could remodel the immunosuppressive microenvironment of triple negative breast cancer and facilitate the checkpoint blockade immunotherapy.
  • ||||||||||  luminespib (AUY922) / Ligand, tanespimycin (BMS-722782) / BMS
    Preclinical, Journal:  Hsp90 inhibitors induce the unfolded protein response in bovine and mice lung cells. (Pubmed Central) -  Jun 10, 2021   
    Similar events occurred in the lungs of mice treated with AUY-922. Thus, our study demonstrates that Hsp90 inhibition triggers the activities of the unfolded protein response, and suggests that this molecular machinery contributes in the protective action of Hsp90 inhibitors in the lung microvasculature.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting. (Pubmed Central) -  May 29, 2021   
    HSP90 ATPase activity inhibition assay were conducted where compound 5d exhibited the best IC with 1.58 μM compared to Tanespimycin (IC = 2.17 μM)...Molecular docking studies suggested mode of interaction to HSP90 via hydrogen bonding. ADME properties prediction of the active compounds suggested that they could be used as orally absorbed anticancer drug candidates.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Regulation of the EGFR Pathway by HSP90 Is Involved in the Pathogenesis of Cushing's Disease. (Pubmed Central) -  May 21, 2021   
    The HSP90 inhibitor 17-AAG reduced the viability and secretory function of human pituitary ACTH-secreting tumor cells, and tumor cells carrying the USP8 mutant were more sensitive to 17-AAG than tumor cells carrying wild-type USP8. 17-AAG could be a potential treatment option for CD.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Clinical, Journal:  Quantitative Proteomics Reveals that Hsp90 Inhibition Dynamically Regulates Global Protein Synthesis in Leishmania mexicana. (Pubmed Central) -  May 13, 2021   
    The classical Hsp90 inhibitor tanespimycin has shown potent antileishmanial activity...Using a combination of mass spectrometry-based quantitative proteomics and chemical and metabolic labeling, we provide the first protein-level evidence that Hsp90 inhibition affects global protein synthesis in Leishmania We also provide the precise relative quantitative changes in the expressions of hundreds of affected proteins as functions of both the concentration and duration of the inhibitor treatment. We find that Leishmania regulates its ribosomal proteins under Hsp90 inhibition while a set of virulence factors and chaperones are preferentially synthesized.
  • ||||||||||  cyclosporine / Generic mfg.
    Journal:  Tornadic Shear Stress Induces a Transient, Calcineurin-Dependent Hypervirulent Phenotype in Mucorales Molds. (Pubmed Central) -  Apr 10, 2021   
    Here, we describe that tornadic shear stress challenge transiently induces a hypervirulent phenotype in various pathogenic Mucorales species but not in other molds known to cause wound infections. Pharmacological and genetic inhibition of calcineurin signaling abrogated hypervirulence in shear stress-challenged Mucorales, encouraging further evaluation of (topical) calcineurin inhibitors to improve therapeutic outcomes of NMM after combat-related blast injuries or violent storms.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  SARS-CoV-2 infection remodels the host protein thermal stability landscape. (Pubmed Central) -  Feb 23, 2021   
    Pharmacological inhibition of host proteins displaying altered thermal stability or abundance during infection suppressed SARS-CoV-2 replication. Overall, this work serves as a framework for expanding TPP workflows to globally important human pathogens that require high biosafety containment and provides deeper resolution into the molecular changes induced by SARS-CoV-2 infection.
  • ||||||||||  tanespimycin (BMS-722782) / BMS
    Journal:  Heat shock proteins as a new, promising target of multiple myeloma therapy. (Pubmed Central) -  Jan 23, 2021   
    Effects were more pronounced when combined with bortezomib. It seems that enriching the range of anti-myeloma drugs with HSP inhibitors may be the next step in the future of extending life of patients with multiple myeloma.