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DRUG:

elesclomol (STA-4783)

i
Other names: STA-4783
Company:
Madrigal Pharma
Drug class:
Apoptosis stimulant, Reactive oxygen species stimulant, HSP70 stimulant
3d
PEGylated Elesclomol@Cu(Ⅱ)-based Metal‒organic framework with effective nanozyme performance and cuproptosis induction efficacy for enhanced PD-L1-based immunotherapy. (PubMed, Mater Today Bio)
Furthermore, combining ES@Cu(Ⅱ)-MOF with an anti-programmed cell death-ligand 1 (PD-L1) antibody converted the immunosuppressive tumor microenvironment to an immunogenic microenvironment, thus effectively inhibiting breast tumor growth. Overall, this work provides an innovative approach utilizing nanozymes to facilitate cuproptosis for cancer treatment, which potentially enhances the effectiveness of immune checkpoint inhibitor-based immunotherapy.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase)
|
elesclomol (STA-4783)
4d
Pan-cancer analysis of oncogenic role of CEP55 and experiment validation in clear cell renal cell carcinoma. (PubMed, Sci Rep)
We also used Gene Set Cancer Analysis (GSCA) to predict a serious of small molecule CEP55 targeted drugs, such as AZ628, SB52334, SB590885, A-770,041, AZD7762, Elesclomol, panobinostat, BRD-A94377914, and LRRK2-IN-1. Our study indicated that CEP55 overexpression in most caner types was associated with poor prognosis. Notably, CEP55 was closely relevant to immune cell infiltration and impacted the response to immunotherapy and small molecule drugs against cancers.
Journal • PD(L)-1 Biomarker • IO biomarker • Pan tumor
|
CD4 (CD4 Molecule) • CCNA2 (Cyclin A2) • PCNA (Proliferating cell nuclear antigen) • CDK1 (Cyclin-dependent kinase 1) • KIF11 (Kinesin Family Member 11) • CEP55 (Centrosomal Protein 55) • LRRK2 (Leucine Rich Repeat Kinase 2)
|
Farydak (panobinostat) • AZ 628 • elesclomol (STA-4783) • AZD-7762 • SB-590885
5d
CDH2 and CDH13 as potential prognostic and therapeutic targets for adrenocortical carcinoma. (PubMed, Cancer Biol Ther)
Foretinib and elesclomol were predicted to exert strong inhibitory effects on SW13 cells by inhibiting the expression of CDH2 and CDH13. These data indicate that CDH2 and CDH13 are promising targets for precise treatment of ACC and may serve as new biomarkers for ACC prognosis.
Journal • PD(L)-1 Biomarker • IO biomarker
|
CDH2 (Cadherin 2)
|
CDH1 expression
|
elesclomol (STA-4783) • foretinib (GSK1363089)
21d
Signaling Mechanism of Cuproptosis Activating cGAS-STING Immune Pathway. (PubMed, JACS Au)
With Cu-DPPZ-Py+ and Cu-Elesclomol, there is strong evidence that the triggering cuproptosis significantly drives mitochondrial DNA (mtDNA) release to activate innate immunity via cyclic GMP-AMP synthase-stimulation of interferon genes (cGAS-STING), which can improve T cell antitumor immunity in vivo. By contrast, it is observed that Cu-DPPZ-Ph treated tumor cells could release intracellular caspase-3, resulting in apoptosis-associated immunosuppression. This study supports insights into how cuproptosis bridges cGAS-STING immune pathways, contributing to the development of cuproptosis-based antitumor immunotherapy.
Journal
|
STING (stimulator of interferon response cGAMP interactor 1) • CASP3 (Caspase 3) • CGAS (Cyclic GMP-AMP Synthase)
|
elesclomol (STA-4783)
1m
Development and Validation of a Comprehensive Prognostic and Depression Risk Index for Gastric Adenocarcinoma. (PubMed, Int J Mol Sci)
With the Genomics of Drug Sensitivity in Cancer database, we found that the gastric adenocarcinoma patients with high risk-score may be sensitive to Pazopanib, XMD8.85, Midostaurin, HG.6.64.1, Elesclomol, Linifanib, AP.24534, Roscovitine, Cytarabine, and Axitinib. The gene signature consisting of the NDUFA4L2, ANKRD45, and AQP3 genes is a promising biomarker to distinguish the prognosis, the molecular and immune characteristics, the depressive risk, and the therapy candidates for gastric adenocarcinoma patients.
Journal
|
NDUFA4L2 (NDUFA4 Mitochondrial Complex Associated Like 2)
|
cytarabine • Iclusig (ponatinib) • pazopanib • Rydapt (midostaurin) • Inlyta (axitinib) • elesclomol (STA-4783) • linifanib (ABT-869) • seliciclib (CYC202)
1m
Statins, Cholesterol and Cognitive Decline in Alzheimer's (clinicaltrials.gov)
P=N/A, N=1000, Not yet recruiting, Karolinska Institutet
New trial
|
elesclomol (STA-4783)
2ms
Cuproptosis in microsatellite stable colon cancer cells affects the cytotoxicity of CD8+T through the WNT signaling pathway. (PubMed, Chem Biol Interact)
The study developed an MSS CC cuproptosis model using 50 nM elesclomol and 1 μM CuCl2...Cuproptosis in MSS CC cells enhances the cytotoxicity of CD8+ T cells, which may be achieved through downregulation of the WNT signaling pathway and decreased expression of PD-L1. In the future, drugs that can induce cuproptosis may be a promising approach to improve MSS CC immunotherapy.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8)
|
PD-L1 expression
|
elesclomol (STA-4783)
2ms
AB017. NFκB1 regulates FDX1 to facilitate elesclomol-induced cuproptosis against glioblastoma. (PubMed, Chin Clin Oncol)
Elesclomol inhibits glioblastoma development via inducing cuproptosis, regulated by NFκB1/FDX1 axis.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • SLC7A11 (Solute Carrier Family 7 Member 11) • ATP7A (ATPase Copper Transporting Alpha) • DLAT (Dihydrolipoamide S-Acetyltransferase) • FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783)
3ms
Exploring the prognosis value, immune correlation, and drug responsiveness prediction of homeobox C6 (HOXC6) in lung adenocarcinoma. (PubMed, Discov Oncol)
Taken together, there is a great potential for HOXC6 to become a prognosis biomarker and contribute to develop treatment strategies for LUAD patients. Further mechanism exploration and drug development for HOXC6 are needed.
Journal
|
HOXC6 (Homeobox C6)
|
docetaxel • cytarabine • Torisel (temsirolimus) • sirolimus • Zolinza (vorinostat) • elesclomol (STA-4783)
3ms
The signature genes of cuproptosis associates with tumor immune microenvironment and predicts prognosis in kidney renal clear cell carcinoma. (PubMed, Front Oncol)
Cell experiments were conducted to verify whether FDX1 was involved in cuproptosis of Caki-1 cells induced by Elesclomol...This study provides compelling evidence that cuproptosis is closely linked to the prognosis of KIRC. FDX1 holds promise as a viable biomarker and therapeutic target for assessing the effectiveness of tumor immunotherapy in KIRC.
Journal • IO biomarker
|
FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783)
4ms
A novel signature constructed by cuproptosis-related RNA methylation regulators suggesting downregulation of YTHDC2 may induce cuproptosis resistance in colorectal cancer. (PubMed, Int Immunopharmacol)
We developed a prognostic model constructed by 6 CRRMRs to assess overall survival and immune microenvironment of CRC patients. YTHDC2 might regulate cuproptosis in multiple ways.
Journal • Tumor mutational burden
|
TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • YTHDC2 (YTH N6-Methyladenosine RNA Binding Protein C2)
|
elesclomol (STA-4783)
4ms
Dysregulated Wnt/β-catenin signaling confers resistance to cuproptosis in cancer cells. (PubMed, Cell Death Differ)
Knockdown of TCF4 or pharmacological Wnt/β-catenin blockade increased the sensitivity of CSCs to elesclomol-Cu-induced cuproptosis. These findings reveal a link between copper homeostasis regulated by the Wnt/β-catenin pathway and cuproptosis sensitivity, and suggest a precision medicine strategy for cancer treatment through selective cuproptosis induction.
Journal
|
TCF4 (Transcription Factor 4)
|
elesclomol (STA-4783)
5ms
Copper(II)-Based Nano-Regulator Correlates Cuproptosis Burst and Sequential Immunogenic Cell Death for Synergistic Cancer Immunotherapy. (PubMed, Biomater Res)
To trigger cuproptosis, copper-ionophore elesclomol (ES) had to be employed for the copper-transporting-mediated process...This enabled an increased infiltration of cytotoxic CD8+ T cells and consequently enhanced antitumor immune responses for successfully suppressing fibrosarcoma growth. Thus, the copper(II)-based metal-organic framework nano-regulator offered a promising approach for inducing cuproptosis and cuproptosis-stimulated ICD for cancer immunotherapy.
Journal
|
CD8 (cluster of differentiation 8)
|
elesclomol (STA-4783)
5ms
Long non-coding RNAs in ferroptosis and cuproptosis impact on prognosis and treatment in hepatocellular carcinoma. (PubMed, Clin Exp Med)
Finally, we validated the accuracy of FCRLs in hepatocellular carcinoma cell lines using induction agents (elesclomol and erastin). Cellular assays revealed significant changes in the expression of AC019080.5, AC145207.5, MIR210HG, and LINC01063 in HCC cell lines following the addition of ferroptosis and cuproptosis inducers. We created a signature of four FCRLs that accurately predicted survival in HCC patients, laid the foundation for basic research related to ferroptosis and cuproptosis in hepatocellular carcinoma, and provided therapeutic recommendations for HCC patients.
Journal • IO biomarker
|
MIR210HG (MIR210 Host Gene)
|
elesclomol (STA-4783) • erastin
5ms
Enzalutamide Sensitizes Castration-Resistant Prostate Cancer to Copper-Mediated Cell Death. (PubMed, Adv Sci (Weinh))
Here, the synergistic induction of copper-dependent cell death (cuproptosis) in CRPC cells is reported by enzalutamide and copper ionophores (elesclomol/disulfiram). Importantly, enzalutamide significantly enhances copper ionophore-mediated cytotoxicity in enzalutamide-resistant cells. Collectively, these findings indicate that enzalutamide and copper ionophores synergistically induce cuproptosis, offering a promising therapeutic avenue for CRPC, potentially including enzalutamide-resistant cases.
Journal
|
PTEN (Phosphatase and tensin homolog) • FDX1 (Ferredoxin 1)
|
Xtandi (enzalutamide capsule) • elesclomol (STA-4783)
6ms
Ferritinophagy mediates adaptive resistance to EGFR tyrosine kinase inhibitors in non-small cell lung cancer. (PubMed, Nat Commun)
Osimertinib (Osi) is a widely used epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Combining Osi with elesclomol, a copper ion ionophore, significantly increases the efficacy of Osi, with no additional toxicity. Altogether, this study reveals the mechanisms of NCOA4-mediated ferritinophagy in Osi adaptive resistance and introduces a promising new therapy of combining copper ionophores to improve its initial efficacy.
Journal
|
EGFR (Epidermal growth factor receptor) • NCOA4 (Nuclear Receptor Coactivator 4)
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Tagrisso (osimertinib) • elesclomol (STA-4783)
6ms
Elesclomol-copper synergizes with imidazole ketone erastin by promoting cuproptosis and ferroptosis in myelodysplastic syndromes. (PubMed, Biomed Pharmacother)
Cell viability assays showed that the glutathione and its precursor N-acetylcysteine could significantly rescue the cell death under either mono or combination treatment, demonstrating that GSH acts at the crossing point in the regulation network of cuproptosis and ferroptosis. Significantly, the reconstitution of xCT expression and knockdown of FDX1 cells have been found to contribute to the tolerance of mono treatment but have little recovery impact on the combined treatment. Collectively, these findings suggest that a synergistic interaction leading to the induction of multiple programmed cell death pathways could be a promising approach to enhance the effectiveness of therapy for MDS.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase) • FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783) • erastin
7ms
A cuproptosis-related signature predicts prognosis and indicates cross-talk with immunocyte in ovarian cancer. (PubMed, Discov Oncol)
This study constructed a new cuproptosis-related gene signature that has a good prognostic capacity in assessing the outcome of OC patients. This study enhances our understanding of cuproptosis associated with ovarian cancer aggressiveness, cross-talk with immunocytes, and serves as a novel chemotherapy strategy.
Journal
|
KIF26B (Kinesin Family Member 26B)
|
cisplatin • elesclomol (STA-4783)
7ms
Disulfiram mediated anti-tumour effect in pituitary neuroendocrine tumours by inducing cuproptosis. (PubMed, Int Immunopharmacol)
The present study revealed copper ionophores as a potential class of drugs for PitNET treatment. DSF induced PitNET cell death via cuproptosis and might be a promising option for PitNET therapy.
Journal
|
SSTR (Somatostatin Receptor)
|
elesclomol (STA-4783)
7ms
Elesclomol-Cu Induces Cuproptosis in Human Acute Myeloid Leukemia Cells (PubMed, Zhongguo Shi Yan Xue Ye Xue Za Zhi)
ES-Cu can induce cuproptosis in AML cells, which provides a new idea for the treatment of AML.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase) • DPYD (Dihydropyrimidine Dehydrogenase) • FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783)
8ms
Validation of CDC45 as a novel biomarker for diagnosis and prognosis of gastric cancer. (PubMed, PeerJ)
In a comprehensive the drug susceptibility analysis, we found that patients with high expression of CDC45 had high sensitivity to various chemotherapeutic agents, among which 5-fluorouracil, docetaxel, cisplatin, and elesclomol were most evident. Enrichment analysis revealed that CDC45 and its associated genes may play crucial roles in muscle biofunction, whereas GSEA demonstrated significant enrichment of gene sets pertaining to G protein-coupled receptor ligand binding and G alpha (i) signaling events. Our study elucidates that upregulation of CDC45 is intricately associated with immune cell infiltration and holds promising potential as a favorable prognostic marker and a novel diagnostic biomarker for GC.
Journal
|
CDC45 (Cell Division Cycle 45)
|
cisplatin • docetaxel • 5-fluorouracil • elesclomol (STA-4783)
9ms
Protein phosphatase 1 regulatory subunit 15 A promotes translation initiation and induces G2M phase arrest during cuproptosis in cancers. (PubMed, Cell Death Dis)
In our study, we demonstrated that elesclomol, as a carrier of copper ions, caused an upregulation of protein phosphatase 1 regulatory subunit 15 A (PPP1R15A), which plays a role in regulating substrate selectivity of protein phosphatase 1 during cuproptosis. Mechanistically, we investigated that PPP1R15A activated translation initiation by dephosphorylating eukaryotic translation initiation factor 2 subunit alpha at the S51 residue through protein phosphatase 1 and phosphorylating eukaryotic translation initiation factor 4E binding protein 1 at the T70 residue. In addition, PPP1R15A reduced H3K4 methylation by altering the phosphorylation of histone methyltransferases, which led to the silencing of MYC and G2M phase arrest.
Journal
|
EIF4EBP1 (Eukaryotic translation initiation factor 4E binding protein 1) • PPP1R15A (Protein Phosphatase 1 Regulatory Subunit 15A) • EIF2S1 (Eukaryotic Translation Initiation Factor 2 Subunit Alpha)
|
elesclomol (STA-4783)
10ms
Redox modulation of oxidatively-induced DNA damage by ascorbate enhances both in vitro and ex-vivo DNA damage formation and cell death in melanoma cells. (PubMed, Free Radic Biol Med)
Finally, we show that ascorbate serves to enhance the oxidising effects of the MM therapeutic drug Elesclomol in both established MM cells in vitro and primary cell cultures ex vivo. Together, these results suggest that ascorbate selectively enhances DNA damage and cell-killing in MM cells. This raises the option of incorporating ascorbate into clinical oxidative therapies to treat MM.
Preclinical • Journal
|
CAT (Catalase)
|
elesclomol (STA-4783)
11ms
Cuproptosis/OXPHOS Tendency Prediction of Prognosis and Immune Microenvironment of Esophageal Squamous Cell Carcinoma: Bioinformatics Analysis and Experimental Validation. (PubMed, Gene)
Our study revealed the relationship between OXPHOS and tendency of cuproptosis in ESCC, and malignant cells with this characteristic exerted immunosuppressive signals and indicated poor prognosis. Furthermore, we constructed the constructed the regulatory network in high cuproptosis-OXPHOS ESCC and identified HMGA1 as a potential regulator molecule of cuproptosis mediated by elesclomol.
Journal
|
IGFBP2 (Insulin-like growth factor binding protein 2) • RASGRF1 (Ras Protein Specific Guanine Nucleotide Releasing Factor 1) • CCDC25 (Coiled-Coil Domain Containing 25)
|
erlotinib • dasatinib • Bosulif (bosutinib) • elesclomol (STA-4783)
11ms
Transcriptomic correlates of cell cycle checkpoints with distinct prognosis, molecular characteristics, immunological regulation, and therapeutic response in colorectal adenocarcinoma. (PubMed, Front Immunol)
In addition, GSE173839, GSE25066, GSE41998, and GSE194040 dataset analyses of the underlying CCC signature suggested that durvalumab with olaparib and paclitaxel, taxane-anthracycline chemotherapy, neoadjuvant cyclophosphamide/doxorubicin with ixabepilone or paclitaxel, and immunotherapeutic strategies might be suitable for COAD patients with higher CCC score. Eventually, the GDSC database analysis showed that lower CCC scores were likely to be more sensitive to 5-fluorouracil, bosutinib, gemcitabine, gefitinib, methotrexate, mitomycin C, and temozolomide, while patients with higher CCC score seemed to have a higher level of sensitivity to bortezomib and elesclomol. The novel CCC signature exhibited a good ability for prognosis prediction for COAD patients, and the CCC score was found to be highly correlated with molecular features, immune-related characteristics, and therapeutic responses, which would greatly promote clinical management and precision medicine for COAD.
Journal • PARP Biomarker • PD(L)-1 Biomarker • IO biomarker
|
NBN (Nibrin Nijmegen Breakage Syndrome 1 (Nibrin)) • MAD1L1 (Mitotic Arrest Deficient 1 Like 1) • ZNF207 (Zinc Finger Protein 207) • CDK5RAP2 (CDK5 Regulatory Subunit Associated Protein 2)
|
Lynparza (olaparib) • Imfinzi (durvalumab) • gefitinib • gemcitabine • paclitaxel • 5-fluorouracil • temozolomide • bortezomib • doxorubicin hydrochloride • cyclophosphamide • Bosulif (bosutinib) • methotrexate • mitomycin • Ixempra (ixabepilone) • elesclomol (STA-4783)
11ms
Construction of a prognostic model for lung adenocarcinoma based on m6A/m5C/m1A genes. (PubMed, Hum Mol Genet)
Based on the m6A/m5C/m1A-related genes in LUAD, LUAD patients were divided into 2 subtypes, and a m6A/m5C/m1A-related LUAD prognostic model was constructed to provide a reference for the prognosis prediction of LUAD.
Journal
|
CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
|
Alecensa (alectinib) • Alunbrig (brigatinib) • irinotecan • Torisel (temsirolimus) • saracatinib (AZD0530) • elesclomol (STA-4783) • Emcyt (estramustine)
12ms
LINC02362/hsa-miR-18a-5p/FDX1 axis suppresses proliferation and drives cuproptosis and oxaliplatin sensitivity of hepatocellular carcinoma. (PubMed, Am J Cancer Res)
Furthermore, LINC02362 knockdown led to a reduction in copper concentration and resistance to elesclomol-Cu. We also discovered that augmenting the LINC02362/hsa-miR-18a-5p/FDX1 axis could bolster the sensitivity of HCC to oxaliplatin through cuproptosis. This work presents the LINC02362/hsa-miR-18a-5p/FDX1 axis as a novel pathway that triggers cuproptosis and enhances the sensitivity of HCC to oxaliplatin, presenting a promising therapeutic avenue to combat oxaliplatin resistance in HCC.
Journal
|
MIR18A (MicroRNA 18a) • FDX1 (Ferredoxin 1)
|
oxaliplatin • elesclomol (STA-4783)
1year
A Polymeric Hydrogel to Eliminate Programmed Death-Ligand 1 for Enhanced Tumor Radio-Immunotherapy. (PubMed, ACS Nano)
Herein, we develop a sodium alginate hydrogel consisting of elesclomol-Cu and galactose to induce persistent cuproptosis, leading to the reduction of PD-L1 for radio-immunotherapy of colon tumors...Consequently, the sensitization of tumor to radiotherapy and immunotherapy is significantly improved, further prolonging the survival of tumor-bearing mice in both local and metastatic tumors. Our study introduces an approach that combines cuproptosis with immunotherapy and radiotherapy.
Journal
|
PD-L1 (Programmed death ligand 1) • DLAT (Dihydrolipoamide S-Acetyltransferase)
|
elesclomol (STA-4783)
1year
MELK promotes HCC carcinogenesis through modulating cuproptosis-related gene DLAT-mediated mitochondrial function. (PubMed, Cell Death Dis)
Moreover, the above changes of MELK to HCC were abolished by elesclomol. In conclusion, MELK enhanced the levels of the cuproptosis-related signature(CRS) gene DLAT (especially the proportion of DLAT monomer) by activating the PI3K/mTOR pathway, thereby promoting elesclomol drug resistance, altering mitochondrial function, and ultimately promoting HCC progression.
Journal
|
MELK (Maternal Embryonic Leucine Zipper Kinase) • DLAT (Dihydrolipoamide S-Acetyltransferase)
|
elesclomol (STA-4783)
1year
Lactylation of METTL16 promotes cuproptosis via mA-modification on FDX1 mRNA in gastric cancer. (PubMed, Nat Commun)
Combining elesclomol with AGK2, a SIRT2-specific inhibitor, induce cuproptosis in gastric tumors in vitro and in vivo. These results reveal the significance of non-histone protein METTL16 lactylation on cuproptosis in tumors. Given the high copper and lactate concentrations in GC, cuproptosis induction becomes a promising therapeutic strategy for GC.
Journal
|
FDX1 (Ferredoxin 1) • METTL16 (Methyltransferase 16, RNA N6-Adenosine)
|
elesclomol (STA-4783) • AGK2
1year
Copper induces neuron-sparing, ferredoxin 1-independent astrocyte toxicity mediated by oxidative stress. (PubMed, J Neurochem)
Given the growing interest in the use of copper in the presence of the ionophore elesclomol (CuES) for the treatment of gliomas, we investigated the effect of this compound on the surround parenchyma-namely neurons and astrocytes in vitro...As neurons express high levels of metallothioneins basally, these results may partially account for their resistance to CuES toxicity. These results demonstrate a unique toxic response to copper in glial cells which contrasts with the cell selectivity profile of zinc, another biologically relevant metal.
Journal
|
FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783)
1year
Exploration of a screening model for intrahepatic cholangiocarcinoma patients prone to cuproptosis and mechanisms of the susceptibility of CD274-knockdown intrahepatic cholangiocarcinoma cells to cuproptosis. (PubMed, Cancer Gene Ther)
Our team's previous research found that ICC patients prone to cuproptosis possessed a more satisfactory long-term prognosis and a more sensitive response to copper carrier Elesclomol...We constructed precise diagnostic and treatment strategies for ICC patients prone to cuproptosis and further explored the intracellular and extracellular mechanisms of ICC cells prone to cuproptosis. Further work with large prospective cohorts will help verify these conclusions.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1)
|
PD-L1 negative
|
elesclomol (STA-4783)
1year
Cuproptosis-related lncRNAs as potential biomarkers of AML prognosis and the role of lncRNA HAGLR/miR-326/CDKN2A regulatory axis in AML. (PubMed, Am J Cancer Res)
Elesclomol promotes the degradation of CDKN2A and inhibits the proliferation of AML cells. Elesclomol combined with si-HAGLR inhibited the AML progression of AML both in vitro and in vivo.
Journal • IO biomarker
|
CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • MIR326 (MicroRNA 326)
|
elesclomol (STA-4783)
over1year
Cuproptosis enhances docetaxel chemosensitivity by inhibiting autophagy via the DLAT/mTOR pathway in prostate cancer. (PubMed, FASEB J)
We treated prostate cancer cell lines with elesclomol-CuCl , as well as with docetaxel. Our findings demonstrated that the cuproptosis-regulated DLAT/mTOR pathway inhibited autophagy and promoted cells in G2/M phase retention, thus enhancing the chemosensitivity to docetaxel. This discovery may provide an effective therapeutic option for treating advanced prostate cancer by inhibiting the chemotherapeutic resistance to docetaxel.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase)
|
docetaxel • elesclomol (STA-4783)
over1year
FDX1 inhibits thyroid cancer malignant progression by inducing cuprotosis. (PubMed, Heliyon)
Induction of cuprotosis by elesclomol (ES) significantly repressed the in vitro and in vivo growth of thyroid cancer cells, simultaneously elevated Cu level and expression of FDX1, whereas depletion of FDX1 abolished these effects. Knockdown of FDX1 decreased the lipoylation level of DLAT and DLST in thyroid cancer cells, alleviated cuprotosis-induced cell death, simultaneously upregulated the levels of PA and α-KG. These findings demonstrated that FDX1 promotes the cuprotosis of thyroid cancer cells via regulating the lipoylation of DLAT.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase) • FDX1 (Ferredoxin 1)
|
elesclomol (STA-4783)
over1year
Identification of a novel prognostic signature composed of 3 cuproptosis-related transcription factors in colon adenocarcinoma. (PubMed, Genes Genomics)
Our research has identified a new prognostic biomarker and provides some innovative insights into the diagnosis and therapy of patients with COAD.
Journal
|
E2F3 (E2F transcription factor 3)
|
elesclomol (STA-4783)
over1year
Characterization of a cuproptosis-related signature to evaluate immune features and predict prognosis in colorectal cancer. (PubMed, Front Oncol)
Elesclomol, a potent copper ionophore, significantly altered expressions of seven CRGs in CRCs, indicating their relationship with cuproptosis. The cuproptosis-related gene signature could serve as a potential prognostic predictor for colorectal cancer patients and may offer novel insights into clinical cancer therapeutics.
Journal
|
elesclomol (STA-4783)
over1year
In vitro and in vivo characterization of [Cu][Cu(elesclomol)] as a novel theranostic agent for hypoxic solid tumors. (PubMed, Eur J Nucl Med Mol Imaging)
To the best of our knowledge, this is the first time that ES is radiolabeled with [Cu]CuCl to [Cu][Cu(ES)]. We demonstrated superior therapeutic effects of [Cu][Cu(ES)] compared to [Cu][Cu(ATSM)] and [Cu]CuCl and that [Cu][Cu(ES)]-PET is feasible. [Cu][Cu(ES)] is a promising theranostic agent for hypoxic solid tumors.
Preclinical • Journal
|
elesclomol (STA-4783)
over1year
DLAT as a Cuproptosis Promoter and a Molecular Target of Elesclomol in Hepatocellular Carcinoma. (PubMed, Curr Med Sci)
Cuproptosis and DLAT as a promising biomarker could help to determine the prognosis of HCC and may offer novel insights for effective treatment.
Journal
|
DLAT (Dihydrolipoamide S-Acetyltransferase)
|
elesclomol (STA-4783)
over1year
Ferroptosis inducers enhanced cuproptosis induced by copper ionophores in primary liver cancer. (PubMed, J Exp Clin Cancer Res)
Our findings proposed that combination of ferroptosis inducers and copper ionophores to co-targeting ferroptosis and cuproptosis could be a novel therapeutic strategy for primary liver cancer.
Journal
|
FDX1 (Ferredoxin 1)
|
sorafenib • elesclomol (STA-4783)
over1year
Cuproptosis Induced by ROS Responsive Nanoparticles with Elesclomol and Copper Combined with αPD-L1 for Enhanced Cancer Immunotherapy. (PubMed, Adv Mater)
Additionally, NP@ESCu was further combined with anti-programmed cell death protein ligand-1 antibody (?PD-L1). This study provides the first report of combining nanomedicine that can induce cuproptosis with ?PD-L1 for enhanced cancer therapy, thereby providing a novel strategy for future cancer therapy.
Journal
|
elesclomol (STA-4783)