- |||||||||| 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.
- |||||||||| 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
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.
- |||||||||| tanespimycin (BMS-722782) / BMS
Journal: Identification of Subtype-Specific Metastasis-Related Genetic Signatures in Sarcoma. (Pubmed Central) - Nov 1, 2020 We also identified Tanespimycin as a drug exerting inhibitory effects on metastatic LMS subtype and therefore can serve a potential treatment for this type of sarcoma. These results provide new insights into the pathogenesis, diagnosis, treatment, and prognosis of sarcomas and provide new directions for further study of sarcoma.
- |||||||||| Journal, Gene Expression Profile, PARP Biomarker: Computational Drug Repositioning for Gastric Cancer using Reversal Gene Expression Profiles. (Pubmed Central) - Sep 21, 2020
Meanwhile, GC-related genes such as PLOD3, COL4A1, UBE2C, MIF, and PRPF5 were identified as having gene expression profiles that can be reversed by drugs. These findings support the use of a computational reversal gene expression approach to identify new drug candidates that can be used to treat GC.
- |||||||||| sirolimus / Generic mfg., tanespimycin (BMS-722782) / BMS
Journal: The dual functions of α-tubulin acetylation in cellular apoptosis and autophage induced by tanespimycin in lung cancer cells. (Pubmed Central) - Aug 11, 2020 According to results of RNA interference, acetyltransferase TAT1, deacetylase HDAC6 and Hsp90 modulated the expression level of α-tubulin acetylation. We have elucidated that acetylation of α-tubulin induced by tanespimycin has dual functions in cellular apoptosis and autophage and the level of α-tubulin acetylation reaches a degree Calu-1 cells undergo cell apoptosis rather than autophage, implying that the level of acetylated α-tubulin may determine cell fate for survival or apoptosis.
- |||||||||| tanespimycin (BMS-722782) / BMS
Journal: Transcriptomics-Based Screening Identifies Pharmacological Inhibition of Hsp90 as a Means to Defer Aging. (Pubmed Central) - Jun 26, 2020 Testing the top candidates in C. elegans, we identified two Hsp90 inhibitors, monorden and tanespimycin, which extended the animals' lifespan and improved their health...Consistently, monorden treatment improved the survival of C. elegans under proteotoxic stress, and its benefits depended on the cytosolic unfolded protein response-inducing transcription factor HSF-1. Taken together, our method represents an innovative geroprotector screening approach and was able to identify a class that acts by improving protein homeostasis.
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