tanespimycin (BMS-722782) / BMS - LARVOL DELTA

A small-molecule HSP90 inhibitor, NVP-HSP990, alleviates rotavirus infection. (PubMed, J Virol) - "In this study, we demonstrated that NVP-HSP990, a novel small-molecule heat shock protein 90 (HSP90) inhibitor, inhibited RV infection with a fascinatingly higher selectivity index compared to conventional HSP90 inhibitors like geldanamycin and its derivative tanespimycin (17-allylamino-17-demethoxygeldanamycin [17-AAG])...As a result, NVP-HSP990 significantly alleviated the severity of RV-induced diarrhea. Given its excellent oral efficacy and systemic penetration previously reported, NVP-HSP990 emerges as a promising HSP90-targeted candidate capable of addressing both intestinal and possible extraintestinal RV infections, which also repositions HSP90 inhibition as a viable strategy in RV management."

Journal • Infectious Disease • Inflammation • Rotavirus Infections • CDC37 • IL17A

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."

IO biomarker • Journal • Metabolic Disorders • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • Targeted Protein Degradation • CDC37 • GPX4 • HSP90AA1

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."

IO biomarker • Journal • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • JAG1 • PLAU

Targeting treatment-resistant Systemic Lupus Erythematosus through transcriptome-informed drug repurposing (ACR Convergence 2025) - "To guide precision repurposing, we applied a transcriptome-driven strategy to identify compounds that either mimic the molecular effects of standard therapies or reverse gene expression profiles associated with treatment resistance. Paired whole-blood transcriptomes from 31 SLE patients treated with rituximab (n=8), belimumab (n=13), or cyclophosphamide (n=10) were analyzed to define drug-specific signatures (absolute log₂FC > 0.58, p < 0.05)...Rituximab's signature aligned with mTOR blockers (everolimus, dactolisib), PI3K inhibitors (PIK-75, ZSTK474), JAK2 inhibitors (fedratinib) and agents downregulating the p38-MAPK pathway (OXA)... Our analysis delineates molecular correlates of therapeutic response and identifies candidate drugs capable of emulating molecular effects of standard SLE therapies or reversing gene expression patterns associated with treatment failure, offering a framework for drug repurposing in difficult-to-treat SLE."

IO biomarker • Immunology • Inflammatory Arthritis • Lupus • Systemic Lupus Erythematosus • BCL2 • CDC37

Combination of B-AP15 and HSP90 inhibitor tanespimycin induces ROS-mediated cytotoxicity in human lung cancer cells. (PubMed, BMC Pharmacol Toxicol) - No abstract available

Journal • Lung Cancer • Oncology • Solid Tumor • CDC37

Identification of biomarkers and therapeutic targets of schizophrenia using glutamine metabolism. (PubMed, Asian J Psychiatr) - "This study demonstrates the potential causal association of GM-related genes in SCZ, developed a precise diagnostic model, and proposed novel targeted therapeutic strategies."

Biomarker • Journal • CNS Disorders • Developmental Disorders • Psychiatry • Schizophrenia • SLC1A5

Ginger-derived vesicle-like nanoparticles loaded with curcumin to alleviate ionizing radiation-induced intestinal damage via gut microbiota regulation. (PubMed, Gut Microbes) - "This beneficial effect was attributed to the identified radioprotective metabolites secreted by A. muciniphila, such as tanespimycin (17-AAG), which was demonstrated to deactivate AKT/NF-κB signaling pathway. These findings reveal the impact of plant products on radioprotective microbes and metabolites to target host processes and alleviate IR-induced intestinal damage, shedding light on new insights in the development of novel radioprotectants."

Journal • Gastrointestinal Disorder

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."

Journal • Review • Oncology • CDC37 • HSP90AA1

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."

Biomarker • Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • HSP90AA1

Heat shock protein inhibitors suppress cytokine-induced DUOX2 mRNA and protein expression in human pancreatic cancer cells in a JAK-STAT dependent manner [WITHDRAWN] (AACR 2025) - "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."

IO biomarker • Gastrointestinal Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • CDC37 • DUOX2 • HIF1A • IFNA1 • IL17A • IL4 • MMP7 • PD-L1 • STAT1 • STAT3 • STAT6

High throughput drug screening on head and neck cancer organoids reveals novel therapeutic strategies (COSM 2025) - "Of these, 4 exhibited ≥ 50% selectivity for tumor tissue compared to normal (pracinostat, tanespimycin, SB-743921, and mocetinostat). High-throughput drug screening across eight normal, dysplastic, and HNSCC PDOs revealed protein and epigenetic targeting drugs to have the most proportional hits. Specifically, HSP90 and HDAC inhibitors were most effective within their drug class. Pending dose response experiments and validation across a larger cohort, these results provide potential novel protein and epigenetic targeting strategies as promising approaches in HNSCC."

Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • CDC37 • HSP90AA1

High throughput drug screening on head and neck cancer organoids reveals novel therapeutic strategies (AHNS-COSM 2025) - "Of these, 4 exhibited ≥ 50% selectivity for tumor tissue compared to normal (pracinostat, tanespimycin, SB-743921, and mocetinostat). High-throughput drug screening across eight normal, dysplastic, and HNSCC PDOs revealed protein and epigenetic targeting drugs to have the most proportional hits. Specifically, HSP90 and HDAC inhibitors were most effective within their drug class. Pending dose response experiments and validation across a larger cohort, these results provide potential novel protein and epigenetic targeting strategies as promising approaches in HNSCC."

Head and Neck Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • CDC37 • HSP90AA1

Pharmacological landscape of endoplasmic reticulum stress: uncovering therapeutic avenues for metabolic diseases. (PubMed, Eur J Pharmacol) - "It examines small molecules such as tauroursodeoxycholic acid (TUDCA) and 4-phenylbutyric acid (4-PBA), repurposed drugs like 17-AAG (17-N-allylamino-17demethoxygeldanamycin (tanespimycin)) and berberine, and phytochemicals such as resveratrol and hesperidin. 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."

Journal • Review • Alzheimer's Disease • CNS Disorders • Hepatology • Inflammation • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Movement Disorders • Parkinson's Disease

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 • Endocrine Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Papillary Carcinoma • BRAF • ELF3 • TCF3

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."

IO biomarker • Journal • Preclinical • B Cell Lymphoma • Brain Cancer • CNS Tumor • Embryonal Tumor • Glioma • Lymphoma • Malignant Glioma • Medulloblastoma • Oncology • Rhabdoid Tumor • Sarcoma • Solid Tumor • BCL2 • CDC37 • EIF4E • HSP90AA1 • SMARCA4 • SMARCB1

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 • Immunology • Microsatellite Instability • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Primary Immunodeficiency • MSI • TMB

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 • Oncology • Solid Tumor • AVEN • CDC37 • HSP90AA1

PCSK1N as a tumor size marker and an ER stress response protein in corticotroph pituitary adenomas. (PubMed, J Clin Endocrinol Metab) - "PCSK1N is higher in SCA compared with FCA, and associated with corticotroph cell markers and tumor size. PCSK1N is likely to be part of the adaptive response to ER stress, potentially conferring a survival advantage to the corticotroph tumor cell in conjunction with other proteins."

Journal • Cushing’s Disease • Endocrine Disorders • Oncology • Pituitary Gland Carcinoma • POMC-null Obesity • CDC37 • HSP90AA1 • PCSK1 • TBX1 • TCF19

Mechanisms and efficacy of small molecule "latency promoting agents" to inhibit HIV reactivation ex vivo. (PubMed, JCI Insight) - "While some drugs primarily inhibited one or two steps in HIV reactivation, other drugs (CDK inhibitors, splicing inhibitors, tanespimycin, and triptolide) inhibited multiple stages of HIV transcription and blocked the production of supernatant viral RNA. Dinaciclib, AZD4573, and pladienolide B also appeared to inhibit HIV splicing in unstimulated PBMC. 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."

Journal • Preclinical • Human Immunodeficiency Virus • Infectious Disease

Rational Design of Targeted Gold Nanoclusters with High Affinity to Integrin αvβ3 for Combination Cancer Therapy. (PubMed, Bioconjug Chem) - "The AuNCs were functionalized with anticancer drugs (5-fluorouracil or signaling pathways inhibitors, such as capivasertib, linifanib, tanespimycin, and taselisib) and integrin-targeting peptides (RGD4C or QS13), and we identified the optimal mixed ligand layer to enhance their binding affinity to the cancer cell receptor. Our simulations also revealed that Mn2+ cations are crucial for stabilizing the αvβ3-AuNC complex. These findings demonstrate the potential of carefully designing the surface composition of TNDDSs to optimize their target affinity and specificity."

Journal • Oncology

A Diketopyrrolopyrrole-Based All-in-One Nanoplatform for Self-Reinforcing Mild Photothermal Therapy Cascade Immunotherapy for Tumors. (PubMed, Adv Healthc Mater) - "Subsequently, BDB is co-coated with the heat shock protein (HSP) inhibitor tanespimycin (17-AAG) using the functional amphiphilic polymers DSPE-Hyd-PEG2000-cRGD to form an all-in-one nanoplatform BAG NPs...Additionally, the mild PTT has been demonstrated to induce immunogenic cell death (ICD) and activate a systemic anti-tumor immune response, thereby suppressing both primary and distant tumors. Overall, this study presents a multifunctional nanoplatform designed for precise mild PTT combined with immunotherapy for effective tumor treatment."

Journal • Oncology

Unveiling Immune-related feature genes for Alzheimer's disease based on machine learning. (PubMed, Front Immunol) - "Moreover, utilizing molecular docking analysis, we identified dinaciclib and tanespimycin as promising small molecule drugs targeting RHBDF2 and TNFRSF10B for potential AD treatment. Our findings highlight the diagnostic and therapeutic potential of RHBDF2 and TNFRSF10B in AD management, shedding light on novel strategies for precision medicine in AD."

Biomarker • Journal • Machine learning • Alzheimer's Disease • CNS Disorders • TNFRSF10B

Pharmacokinetics, Dose-Proportionality, and Tolerability of Intravenous Tanespimycin (17-AAG) in Single and Multiple Doses in Dogs: A Potential Novel Treatment for Canine Visceral Leishmaniasis. (PubMed, Pharmaceuticals (Basel)) - "After the administration of multiple doses, Cmax and AUC 0-48 h were 5254 ± 2784 μg/mL and 6850 ± 469 μg/mL × h in plasma and 736 ± 294 μg/mL and 7382 ± 1357 μg/mL × h in tissue transudate, respectively. In conclusion, our results demonstrate the potential of 17-AAG in the treatment of CVL, using a regimen of three doses at 150 mg/m2, since it presents the maintenance of high concentrations in subcutaneous interstitial fluid, low toxicity, and reversible hepatotoxicity."

Journal • PK/PD data • Hepatology • Infectious Disease • CDC37

Mechanistic study of pre-eclampsia and macrophage-associated molecular networks: bioinformatics insights from multiple datasets. (PubMed, Front Genet) - "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."

Journal • Cardiovascular • Gynecology • Hypertension • Renal Disease • NMUR1

Identification of Molecular Mechanisms of Ameloblastoma and Drug Repositioning by Integration of Bioinformatics Analysis and Molecular Docking Simulation. (PubMed, Bioinform Biol Insights) - "Tanespimycin showed the greatest affinity binding value to bind FOS protein. This study presented the underlying molecular mechanisms of disease pathogenesis, biological alteration, and important pathways of AMs and provided a candidate compound, Tanespimycin, targeting FOS protein for the treatment of AMs."

Journal • Oncology