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    DRUG CLASS:

    GSK3β inhibitor

    Related drugs:
    2ms
    Targeting Canonical Wnt-signaling Through GSK-3β in Arrhythmogenic Cardiomyopathy: Conservative or Progressive? (PubMed, J Cardiovasc Transl Res)
    However, varying concerns are reported throughout the literature including the risk of paradoxical arrhythmias, cancer and off-target effects in upstream or downstream pathways. CLINICAL RELEVANCE: In light of the start of the phase 2 TaRGET clinical trial, designed to evaluate the potential therapeutic efficacy of GSK3β inhibition in patients with arrhythmogenic cardiomyopathy, this report aims to review the advantages and disadvantages of this strategy.
    Review • Journal
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    GSK3B (Glycogen Synthase Kinase 3 Beta)
    3ms
    Targeted inhibition of glycogen synthase kinase-3 using 9-ING-41 (elraglusib) enhances CD8 T-cell-reactivity against neuroblastoma cells. (PubMed, Sci Rep)
    Finally, in co-culture experiments with CD8 + T cells, 9-ING-41 improved immune recognition of the neuroblastoma cells, as evidenced by augmented T-cell activation marker levels and T-cell proliferation, which was further enhanced by PD-1 immune checkpoint inhibition. Our preclinical study provides experimental support to further explore the GSK-3β inhibitor 9-ING-41 as an immunomodulatory agent to increase tumor immune recognition in neuroblastoma.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    CD8 (cluster of differentiation 8) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
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    MYCN amplification
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    elraglusib (9-ING-41)
    3ms
    A New Strategy for Adult T-Cell Leukemia Treatment Targeting Glycogen Synthase Kinase-3β. (PubMed, Eur J Haematol)
    GSK-3β functions as an oncogene in ATL and could be a potential therapeutic target.
    Journal
    |
    TP53 (Tumor protein P53) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1) • STAT3 (Signal Transducer And Activator Of Transcription 3) • BIRC5 (Baculoviral IAP repeat containing 5) • BAX (BCL2-associated X protein) • CCNA2 (Cyclin A2) • XIAP (X-Linked Inhibitor Of Apoptosis) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • GSK3B (Glycogen Synthase Kinase 3 Beta) • NFKBIA (NFKB Inhibitor Alpha 2) • BAK1 (BCL2 Antagonist/Killer 1) • JUNB (JunB Proto-Oncogene AP-1 Transcription Factor Subunit)
    |
    MYC expression • MCL1 expression • TP53 expression • BIRC5 expression • BAX expression • CDKN1B expression
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    elraglusib (9-ING-41) • LY2090314
    4ms
    Targeted Therapy With Glycogen Synthase Kinase-3 Inhibition for Arrhythmogenic Cardiomyopathy (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Hamilton Health Sciences Corporation | Initiation date: Apr 2024 --> Oct 2024
    Trial initiation date
    5ms
    Benzimidazole-oxindole hybrids: A novel class of selective dual CDK2 and GSK-3β inhibitors of potent anticancer activity. (PubMed, Arch Pharm (Weinheim))
    In silico docking of the benzimidazole-oxindole hybrid 8v into the catalytic pocket of both CDK2 and GSK-3β revealed its perfect fitting through the formation of hydrogen bonding and hydrophobic interactions with the key amino acids in the binding sites. In addition, in silico absorption, distribution, metabolism, excretion studies proved that 8a-x exhibit satisfactory drug-likeness properties for drug development.
    Journal
    |
    KDR (Kinase insert domain receptor) • CDK1 (Cyclin-dependent kinase 1)
    5ms
    Anti-oxidative stress and cognitive improvement of a semi-synthetic isoorientin-based GSK-3β inhibitor in rat pheochromocytoma cell PC12 and scopolamine-induced AD model mice via AKT/GSK-3β/Nrf2 pathway. (PubMed, Exp Neurol)
    TFGF-18 protects against neuronal cell damage and cognitive impairment by inhibiting oxidative stress via AKT/GSK-3β/Nrf2 pathway.
    Preclinical • Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • BDNF (Brain Derived Neurotrophic Factor)
    |
    MK-2206
    6ms
    Novel selective inhibitors of macropinocytosis-dependent growth in pancreatic ductal carcinoma. (PubMed, Biomed Pharmacother)
    Four compounds (Ivermectin, Tyrphostin A9, LY2090314, and Pyrvinium Pamoate) selectively hampered nutrient scavenging in KRAS-mutated cancer cells. Their ability to impair albumin-dependent proliferation was replicated both in different 2D cell culture systems and 3D organotypic models. These findings provide a new set of compounds specifically targeting macropinocytosis, which could have therapeutic applications in cancer and infectious diseases.
    Journal
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    KRAS (KRAS proto-oncogene GTPase) • AVEN (Apoptosis And Caspase Activation Inhibitor)
    |
    LY2090314
    7ms
    9-ING-41 in Pediatric Patients With Refractory Malignancies. (clinicaltrials.gov)
    P1, N=68, Recruiting, Actuate Therapeutics Inc. | Active, not recruiting --> Recruiting
    Enrollment open
    |
    AFP (Alpha-fetoprotein)
    |
    temozolomide • cyclophosphamide • irinotecan • topotecan • elraglusib (9-ING-41)
    8ms
    Mutational analysis of cfDNA to identify predictive biomarkers in previously untreated patients with metastatic pancreatic cancer receiving the GSK-3 inhibitor elraglusib (9-ING-41) in combination with gemcitabine/nab-paclitaxel in the 1801 phase 2 study. (ASCO 2024)
    Our preliminary analysis of gene mutations in liquid biopsy samples obtained from patients in the ongoing 1801 Part 3B phase 2 trial identified potential predictive biomarkers of clinical outcome in mPDAC patients treated with combination of elraglusib/GnP. Clinical trial information: NCT03678883.
    Combination therapy • P2 data • Clinical • Metastases • Cell-free DNA
    |
    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • DNMT3A (DNA methyltransferase 1) • NOTCH1 (Notch 1) • KMT2C (Lysine Methyltransferase 2C) • NOTCH2 (Notch 2)
    |
    Tempus xF+ Panel
    |
    gemcitabine • albumin-bound paclitaxel • elraglusib (9-ING-41)
    8ms
    Synthetic Lethality between Cohesin and WNT Signaling Pathways in Diverse Cancer Contexts. (PubMed, Cells)
    Finally, LY2090314 caused gene expression dysregulation mainly involving pathways related to transcription regulation, cell proliferation, and chromatin remodeling. For the first time, our work provides the underlying molecular basis for synthetic lethality due to cohesin mutations and suggests that targeting the WNT may be a promising therapeutic approach for tumors carrying mutated cohesin.
    Journal • Synthetic lethality
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    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • STAG2 (Stromal Antigen 2) • RAD21 (RAD21 Cohesin Complex Component) • SMC1A (Structural Maintenance Of Chromosomes 1A)
    |
    MYC expression • STAG2 mutation
    |
    LY2090314
    9ms
    9-ING-41 Plus Carboplatin in Salivary Gland Carcinoma (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, Glenn J. Hanna | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    carboplatin • elraglusib (9-ING-41)
    9ms
    FOLFIRINOX + 9-Ing-41 + Losartan In Pancreatic Cancer (clinicaltrials.gov)
    P2, N=70, Recruiting, Colin D. Weekes, M.D., PhD | Trial completion date: Jul 2024 --> Jul 2026 | Trial primary completion date: Dec 2023 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • elraglusib (9-ING-41)
    11ms
    Actuate 1901: 9-ING-41 in Myelofibrosis (clinicaltrials.gov)
    P2, N=17, Completed, Actuate Therapeutics Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    Jakafi (ruxolitinib) • elraglusib (9-ING-41)
    11ms
    Actuate 1801: 9-ING-41 in Patients With Advanced Cancers (clinicaltrials.gov)
    P2, N=350, Active, not recruiting, Actuate Therapeutics Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    carboplatin • gemcitabine • albumin-bound paclitaxel • irinotecan • pegylated liposomal doxorubicin • lomustine • elraglusib (9-ING-41)
    12ms
    IGC-AD1 Trial on Agitation in Dementia Due to Alzheimer's (clinicaltrials.gov)
    P2, N=164, Recruiting, IGC Pharma LLC | Trial completion date: Dec 2024 --> Jun 2025 | Trial primary completion date: Mar 2024 --> Jun 2025
    Trial completion date • Trial primary completion date
    |
    APOE (Apolipoprotein E) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9)
    1year
    Targeted Therapy With Glycogen Synthase Kinase-3 Inhibition for Arrhythmogenic Cardiomyopathy (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, Hamilton Health Sciences Corporation
    New P2 trial
    1year
    Actuate 1801: 9-ING-41 in Patients With Advanced Cancers (clinicaltrials.gov)
    P2, N=350, Recruiting, Actuate Therapeutics Inc.
    Trial completion date • Trial primary completion date • Metastases
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    carboplatin • gemcitabine • albumin-bound paclitaxel • irinotecan • pegylated liposomal doxorubicin • lomustine • elraglusib (9-ING-41)
    1year
    9-ING-41 Plus Carboplatin in Salivary Gland Carcinoma (clinicaltrials.gov)
    P2, N=35, Recruiting, Glenn J. Hanna | Trial primary completion date: Jan 2024 --> Jun 2024
    Trial primary completion date • Metastases
    |
    carboplatin • elraglusib (9-ING-41)
    1year
    Redundancy of Glycogen Synthase Kinase 3 in Lymphoma Cell Viability, Proliferation, and the Cytotoxicity of Elraglusib (ASH 2023)
    The IC 50 of elraglusib remains similar despite a significant reduction in levels of GSK3, again suggesting that GSK3 is not its cytotoxic target. Importantly, elraglusib retains therapeutic potential in lymphoma however GSK3 is not a surrogate marker for its efficacy and additional studies are required to elucidate the mechanisms through which it mediates its cytotoxic effects.
    PARP Biomarker
    |
    elraglusib (9-ING-41)
    1year
    RiLEY: 9-ING-41 Plus Retifanlimab and Gemcitabine/Nab-Paclitaxel in Patients With Advanced Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=32, Active, not recruiting, Anwaar Saeed | Trial primary completion date: Aug 2024 --> Dec 2024
    Trial primary completion date • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • Zynyz (retifanlimab-dlwr) • elraglusib (9-ING-41)
    1year
    9-ING-41 Plus Carboplatin in Salivary Gland Carcinoma (clinicaltrials.gov)
    P2, N=35, Recruiting, Glenn J. Hanna | Trial primary completion date: Sep 2023 --> Jan 2024
    Trial primary completion date • Metastases
    |
    carboplatin • elraglusib (9-ING-41)
    1year
    IGC-AD1 Trial on Agitation in Dementia Due to Alzheimer's (clinicaltrials.gov)
    P2, N=164, Recruiting, IGC Pharma LLC | Trial completion date: Mar 2024 --> Dec 2024 | Trial primary completion date: Dec 2023 --> Mar 2024
    Trial completion date • Trial primary completion date
    |
    APOE (Apolipoprotein E)
    over1year
    Anti-Alzheimer Activity of Combinations of Cocoa with Vinpocetine or Other Nutraceuticals in Rat Model: Modulation of Wnt3/β-Catenin/GSK-3β/Nrf2/HO-1 and PERK/CHOP/Bcl-2 Pathways. (PubMed, Pharmaceutics)
    The combination of cocoa with nutraceuticals attenuated the AD-mediated deterioration by modulating interrelated pathophysiological pathways, including inflammation, antioxidant responses, GSK-3β-Wnt/β-catenin signaling, ER stress, and apoptosis. These findings provide insights into the intricate pathogenesis of AD and highlight the neuroprotective effects of nutraceuticals through multiple signaling pathways.
    Preclinical • Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • TNFA (Tumor Necrosis Factor-Alpha) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • IL1B (Interleukin 1, beta) • BECN1 (Beclin 1) • WNT3 (Wnt Family Member 3)
    |
    BCL2 expression
    over1year
    Mechanisms of Xiaozheng decoction for anti-bladder cancer effects via affecting the GSK3β/β-catenin signaling pathways: a network pharmacology-directed experimental investigation. (PubMed, Chin Med)
    By employing network pharmacology and conducting in vitro experiments, the mechanism of Xiaozheng decoction's effect against bladder cancer was tentatively elucidated, and its main active ingredients and targets were identified, providing a scientific basis for future research.
    Journal
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    BCL2 (B-cell CLL/lymphoma 2)
    over1year
    A novel FGFR1 inhibitor CYY292 suppresses tumor progression, invasion, and metastasis of glioblastoma by inhibiting the Akt/GSK3β/snail signaling axis. (PubMed, Genes Dis)
    In vivo experiments revealed that CYY292 inhibited U87MG tumor growth more effectively than AZD4547. CYY292 also efficiently reduced GBM cell proliferation and increased survival in orthotopic GBM models. This study further elucidates the function of FGFR1 in the GBM and reveals the effect of CYY292, which targets FGFR1, on downstream signaling pathways directly reducing GBM cell growth, invasion, and metastasis and thus impairing the recruitment, activation, and function of immune cells.
    Journal
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    FGFR1 (Fibroblast growth factor receptor 1)
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    FGFR1 expression
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    fexagratinib (ABSK091)
    over1year
    CD58 acts as a tumor promotor in hepatocellular carcinoma via activating the AKT/GSK-3β/β-catenin pathway. (PubMed, J Transl Med)
    Taken together, CD58 promotes HCC progression and metastasis via activating the AKT/GSK-3β/β-catenin pathway, suggesting that CD58 is a novel prognostic biomarker and therapeutic target for HCC.
    Journal
    |
    CD58 (CD58 Molecule)
    |
    LY294002
    over1year
    Celastrol impairs tumor growth by modulating the CIP2A-GSK3β-MCL-1 axis in gastric cancer cells. (PubMed, Aging (Albany NY))
    Our findings highlight that celastrol has therapeutic potential via inducing apoptosis of gastric cancer cells.
    Journal
    |
    MCL1 (Myeloid cell leukemia 1) • CIP2A (Cellular Inhibitor Of PP2A) • GSK3B (Glycogen Synthase Kinase 3 Beta) • ANXA5 (Annexin A5)
    |
    CIP2A elevation
    over1year
    CCDC85C suppresses colorectal cancer cells proliferation and metastasis through activating GSK-3β and promoting β-catenin degradation. (PubMed, Cell Signal)
    Our results suggested that CCDC85C binds to GSK-3β to promote its activity and facilitates ubiquitination of β-catenin. β-catenin degradation is responsible for the inhibitory effect of CCDC85C on CRC cell proliferation and migration.
    Journal
    |
    GSK3B (Glycogen Synthase Kinase 3 Beta)
    over1year
    Salvigenin Suppresses Hepatocellular Carcinoma Glycolysis and Chemoresistance Through Inactivating the PI3K/AKT/GSK-3β Pathway. (PubMed, Appl Biochem Biotechnol)
    Moreover, Salvigenin strengthened HCC cells' sensitivity to 5-fluorouracil (5-FU) and attenuated HCC 5-FU-resistant cells' resistance to 5-FU...In-vivo assay revealed that Salvigenin hampered the growth and promoted apoptosis of HCC cells in nude mice. Collectively, Salvigenin impedes the aerobic glycolysis and 5-FU chemoresistance of HCC cells by dampening the PI3K/AKT/GSK-3β pathway.
    Journal
    |
    5-fluorouracil
    over1year
    GSK-3 Inhibitor Elraglusib Enhances Tumor-Infiltrating Immune Cell Activation in Tumor Biopsies and Synergizes with Anti-PD-L1 in a Murine Model of Colorectal Cancer. (PubMed, Int J Mol Sci)
    Using paired tumor biopsies, we found that tumor-infiltrating immune cells had a reduced expression of inhibitory immune checkpoints (VISTA, PD-1, PD-L2) and an elevated expression of T-cell activation markers (CTLA-4, OX40L) after elraglusib treatment. These results address a significant gap in knowledge concerning the immunomodulatory mechanisms of GSK-3 inhibitor elraglusib, provide a rationale for the clinical evaluation of elraglusib in combination with immune checkpoint blockade, and are expected to have an impact on additional tumor types, besides CRC.
    Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker • Biopsy • Immune cell
    |
    KDR (Kinase insert domain receptor) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • PD-L2 (Programmed Cell Death 1 Ligand 2) • GDF15 (Growth differentiation factor 15) • CCL2 (Chemokine (C-C motif) ligand 2) • CSF2 (Colony stimulating factor 2) • GZMB (Granzyme B) • CCL22 (C-C Motif Chemokine Ligand 22) • GSDMB (Gasdermin B) • IL1B (Interleukin 1, beta) • RELA (RELA Proto-Oncogene)
    |
    VEGFA elevation • CCL4 elevation • GSDMB expression
    |
    elraglusib (9-ING-41)
    over1year
    RiLEY: 9-ING-41 Plus Retifanlimab and Gemcitabine/Nab-Paclitaxel in Patients With Advanced Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=32, Active, not recruiting, Anwaar Saeed | Trial completion date: Mar 2025 --> Jun 2025 | Trial primary completion date: Mar 2024 --> Aug 2024
    Trial completion date • Trial primary completion date • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • Zynyz (retifanlimab-dlwr) • elraglusib (9-ING-41)
    over1year
    RUNX3 inactivates oncogenic MYC through disruption of MYC/MAX complex and subsequent recruitment of GSK3β-FBXW7 cascade. (PubMed, Commun Biol)
    The evolutionarily conserved Runt domain of RUNX3 interacts directly with the basic helix-loop-helix leucine zipper of MYC, resulting in the disruption of MYC/MAX and MYC/MIZ-1 interactions, enhanced GSK3β-mediated phosphorylation of MYC protein at threonine-58 and its subsequent degradation via the ubiquitin-proteasomal pathway. We therefore uncover a previously unknown mode of MYC destabilization by RUNX3 and provide an explanation as to why RUNX3 inhibits early-stage cancer development in gastrointestinal and lung mouse cancer models.
    Journal
    |
    FBXW7 (F-Box And WD Repeat Domain Containing 7) • RUNX3 (RUNX Family Transcription Factor 3) • GSK3B (Glycogen Synthase Kinase 3 Beta)
    over1year
    Interferon-γ inducible protein 30 promotes the epithelial-mesenchymal transition-like phenotype and chemoresistance by activating EGFR/AKT/GSK3β/β-catenin pathway in glioma. (PubMed, CNS Neurosci Ther)
    The present study suggests that IFI30 is a regulator of the EMT-like phenotype and acts not only as a prognostic marker but also as a potential therapeutic target for temozolomide-resistant glioma.
    Journal
    |
    IFNG (Interferon, gamma) • SNAI2 (Snail Family Transcriptional Repressor 2)
    |
    temozolomide
    over1year
    Deactivation of glycogen synthase kinase-3β by heat shock‑inducible tumor small protein attenuates hyperthermia‑induced pro‑migratory activity in colorectal cancer cells. (PubMed, Int J Oncol)
    HITS knockdown in CRC cells subject to HS showed increased cell migration in wound healing assay, which was decreased by the GSK3β inhibitor AR‑A014418, confirming the anti‑migratory effect of HITS via the deactivation of GSK3β. The present findings indicated that the deactivation of GSK3β sufficiently offset the pro‑migratory effect of hyperthermia via major HSPs in CRC.
    Journal • IO biomarker
    |
    GSK3B (Glycogen Synthase Kinase 3 Beta) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
    over1year
    ADAMDEC1 induces EMT and promotes colorectal cancer cells metastasis by enhancing Wnt/β-catenin signaling via negative modulation of GSK3β. (PubMed, Exp Cell Res)
    Additionally, the blockage of GSK3β by CHIR 99021 markedly abolished the inhibitory effect of ADAMDEC1 knockdown on Wnt/β-catenin signaling. In summary, our findings first indicate that ADAMDEC1 promotes CRC metastasis by negatively regulating GSK3β, activating the Wnt/β-catenin signaling pathway, and inducing EMT, suggesting its potential utility as a therapeutic target for the treatment of metastatic CRC.
    Journal
    |
    CDH1 (Cadherin 1) • VIM (Vimentin) • CDH2 (Cadherin 2) • GSK3B (Glycogen Synthase Kinase 3 Beta)
    |
    CDH1 expression • VIM expression
    over1year
    Chrysomycin A Regulates Proliferation and Apoptosis of Neuroglioma Cells via the Akt/GSK-3β Signaling Pathway In Vivo and In Vitro. (PubMed, Mar Drugs)
    Western blotting revealed that Chr-A disturbed the balance between Bax and Bcl-2, activating a caspase cascade reaction and downregulating the expression of p-Akt and p-GSK-3β, suggesting that Chr-A may contribute to glioblastoma regression modulating in the Akt/GSK-3β signaling pathway to promote apoptosis of neuroglioma cells in vivo and in vitro. Therefore, Chr-A may hold therapeutic promise for glioblastoma.
    Preclinical • Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
    over1year
    Targeting Pro-Survival Autophagy Enhanced GSK-3β Inhibition-Induced Apoptosis and Retarded Proliferation in Bladder Cancer Cells. (PubMed, Curr Oncol)
    Compared to the GSK-3β inhibition alone, its combination with chloroquine (an autophagy inhibitor) significantly reduced BC cell growth. These results suggest that targeting autophagy potentiates GSK-3β inhibition-induced apoptosis and retarded proliferation in BC cells.
    Journal • IO biomarker
    |
    TFEB (Transcription Factor EB 2)
    |
    TFEB translocation
    over1year
    GSK3β-driven SOX2 overexpression is a targetable vulnerability in esophageal squamous cell carcinoma. (PubMed, Oncogene)
    Finally, we demonstrated in tumor xenograft model that GSK3β inhibitor AR-A014418 was effective in suppressing SOX2-positive ESCC tumor progression and inhibited tumor progression cooperatively with chemotherapeutic agent carboplatin. In conclusion, we uncovered a novel role for GSK3β in driving SOX2 overexpression and tumorigenesis and provided evidence that targeting GSK3β may hold promise for the treatment of recalcitrant ESCCs.
    Journal
    |
    CUL4A (Cullin 4A) • SOX2 • GSK3B (Glycogen Synthase Kinase 3 Beta)
    |
    SOX2 overexpression • SOX2 expression
    |
    carboplatin
    over1year
    Chicken Glycogen Synthase Kinase 3β Suppresses Innate Immune Responses and Enhances Avian Leukosis Virus Replication in DF-1 Cells. (PubMed, Microbiol Spectr)
    These results provide new insights into the biofunction of chGSK3β and the virus-host interactions of ALV-J. In addition, this study provides a basis for further research on the function of GSK3 in poultry.
    Journal • IO biomarker
    |
    TLR3 (Toll Like Receptor 3) • GSK3B (Glycogen Synthase Kinase 3 Beta) • IFIH1 (Interferon Induced With Helicase C Domain 1) • OASL (2'-5'-Oligoadenylate Synthetase Like) • IFNB1 (Interferon Beta 1) • IRF7 (Interferon Regulatory Factor 7)
    over1year
    Elraglusib (formerly 9-ING-41) possesses potent anti-lymphoma properties which cannot be attributed to GSK3 inhibition. (PubMed, Cell Commun Signal)
    To confirm the importance of its action on GSK3β, we treated 3 lymphoma cell lines with selective, structurally distinct GSK3 inhibitors: CT99021, SB216763, LY2090314, tideglusib, and elraglusib. These data question GSK3 as the target of elraglusib in lymphoma, and hence the utility of GSK3 expression as a 'stand-alone', therapeutic biomarker in NHL. Video Abstract.
    Journal
    |
    CTNNB1 (Catenin (cadherin-associated protein), beta 1)
    |
    elraglusib (9-ING-41) • LY2090314