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3ms
Identification of biomarkers based on ubiquitin-correlated genes for predicting immune profile and drug sensitivity in lung adenocarcinoma. (PubMed, Front Pharmacol)
The medications TAE684, Cisplatin, and Midostaurin exhibited the largest negative correlation with Riskscore, according to drug sensitivity study. Lastly, we demonstrated through in vitro tests that HEATR1 knockdown markedly reduced LUAD cell survival, migration, and invasion. This study is the first to systematically integrate the ubiquitin pathway with multi-omics data, constructing a robust risk model for LUAD prognosis and immune characteristics, providing a theoretical reference for future exploration of potential biomarkers for LUAD patients' diagnosis.
Journal • IO biomarker
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FAT1 (FAT atypical cadherin 1)
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cisplatin • midostaurin • TAE-684
1year
Prognosis and immunotherapeutic implications of molecular classification of cervical cancer based on immunophenoscore-related genes. (PubMed, J Biomol Struct Dyn)
cluster2 had higher immune cell infiltration levels and better prognosis, with greater sensitivity to Cyclopamine, Imatinib, MG-13, Paclitaxel, PHA-665752, Rapamycin, Sorafenib, Sunitinib, and VX-680. In contrast, cluster3 had higher TTN and PIK3CA mutations and greater sensitivity to AZ628, Dasatinib, Doxorubicin, HG-6-64-1, JQ12, Midostaurin, PF-562271, TAE684, and WH-4-023. In conclusion, we developed a feasible risk score model based on IPS-related genes for cervical cancer prognosis and identified potential drugs for different cervical cancer subtypes.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PD-L2 (Programmed Cell Death 1 Ligand 2)
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PIK3CA mutation
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dasatinib • sorafenib • paclitaxel • imatinib • sunitinib • doxorubicin hydrochloride • midostaurin • sirolimus • AZ 628 • TAE-684 • cyclopamine • RG6146 • benzesulfonate (PF-562271) • PHA665752 • tozasertib (MK-0457)
over1year
Identification of miRNA signature in cancer-associated fibroblast to predict recurrent prostate cancer. (PubMed, Comput Biol Med)
Our findings conducted an integrated bioinformatic analysis to develop a CAFs-related miRNAs model that provides prognostic insights into individualized and precise treatment for prostate adenocarcinoma patients. Downregulation of miR-106b-5p in CAFs significantly suppressed tumor growth, suggesting a potential therapeutic target for cancer treatment.
Journal
|
MIR96 (MicroRNA 96) • MIR106B (MicroRNA 106b) • MIR133B (MicroRNA 133b) • MIR145 (MicroRNA 145) • MIR15B (MicroRNA 15b) • MIR191 (MicroRNA 191) • MIR222 (MicroRNA 222)
|
TAE-684
over1year
Lysophosphatidic Acid Stimulates Mitogenic Activity and Signaling in Human Neuroblastoma Cells through a Crosstalk with Anaplastic Lymphoma Kinase. (PubMed, Biomolecules)
These effects were curtailed by the selective ALK inhibitors NPV-TAE684 and alectinib. LPA enhanced the inhibitory phosphorylation of the tumor suppressor FoxO3a, and this response was impaired by the ALK inhibitors. These results indicate that LPA stimulates mitogenesis of human neuroblastoma cells through a crosstalk with ALK.
Journal
|
ALK (Anaplastic lymphoma kinase) • NTRK (Neurotrophic receptor tyrosine kinase) • ALKAL2 (ALK And LTK Ligand 2)
|
Alecensa (alectinib) • TAE-684
almost2years
Identification and validation of m6A-associated ferroptosis genes in renal clear cell carcinoma. (PubMed, Cell Biol Int)
NIACIN, TAE-684, ROCILETINIB, and others treat ccRCC. We found ccRCC prognostic genes that work. This discovery may lead to new ccRCC treatments.
Journal • IO biomarker
|
EGFR (Epidermal growth factor receptor) • TRIB3 (Tribbles Pseudokinase 3) • CHAC1 (ChaC Glutathione Specific Gamma-Glutamylcyclotransferase 1) • NNMT (Nicotinamide N-Methyltransferase)
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TAE-684 • Xegafri (rociletinib)
2years
Drug repurposing analysis for colorectal cancer through network medicine framework: Novel candidate drugs and small molecules. (PubMed, Cancer Invest)
Based on the gene module, polyethylene glycol, gallic acid, pyrazole, cordycepin, phenothiazine, pantoprazole, cysteamine, indisulam, valinomycin, trametinib, BRD-K81473043, AZD8055, dovitinib, BRD-A17065207, and tyrphostin AG1478 presented as drugs and small molecule candidates previously studied in the CRC. Lornoxicam, suxamethonium, oprelvekin, sirukumab, levetiracetam, sulpiride, NVP-TAE684, AS605240, 480743.cdx, HDAC6 inhibitor ISOX, BRD-K03829970, and L-6307 are proposed as novel drugs and small molecule candidates for CRC.
Journal
|
TERC (Telomerase RNA Component)
|
Mekinist (trametinib) • AZD8055 • TAE-684 • dovitinib (TKI258) • AG1478 • cordycepin (OVI-123) • indisulam (E7070)
almost3years
PI3K pathway mutation predicts an activated immune microenvironment and better immunotherapeutic efficacy in head and neck squamous cell carcinoma. (PubMed, World J Surg Oncol)
The PI3K pathway mutation status could be considered as a potential biomarker to predict better immunotherapeutic efficacy and clinical outcomes after immunotherapy in HNSC patients.
Journal • Tumor mutational burden • IO biomarker
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TMB (Tumor Mutational Burden)
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TMB-H
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PLX4720 • TAE-684 • linsitinib (ASP7487) • BMS-536924
almost3years
Solute Carrier Family 7 Member 11 (SLC7A11) is a Potential Prognostic Biomarker in Uterine Corpus Endometrial Carcinoma. (PubMed, Int J Gen Med)
The half-maximal inhibitory concentration (IC50) results obtained with the cohort from TCGA showed that Z-VAD-FMK (Caspase inhibitor), S-Triphenylmethyl-L-cysteine (S-Trityl-L-cysteine), and TAE684 (ALK inhibitor) had higher IC50 values in low-expression patient (p < 0.05). SLC7A11 overexpression is associated with favorable prognosis of patients with UCEC and is associated with TIICs and the responses to immunotherapy.
Journal • IO biomarker
|
SLC7A11 (Solute Carrier Family 7 Member 11)
|
SLC7A11 expression
|
TAE-684
almost3years
Autocrine EGF and TGF-α promote primary and acquired resistance to ALK/c-Met kinase inhibitors in non-small-cell lung cancer. (PubMed, Pharmacol Res Perspect)
Clinically, NSCLC patients with high expression of EGF and TGF-α developed primary resistance to crizotinib. Furthermore, combined treatment with gefitinib circumvented EGF- and TGF-α-mediated primary and acquired resistance to TAE684/SGX-523. Taken together, these results suggested increased autocrine EGF and TGF-α conferred primary and acquired resistance to ALK/c-Met kinase inhibitors in NSCLC.
Preclinical • Journal
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MET (MET proto-oncogene, receptor tyrosine kinase) • TGFA (Transforming Growth Factor Alpha)
|
EGF overexpression
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Xalkori (crizotinib) • gefitinib • TAE-684 • SGX523
over3years
Distinct Response of Circulating microRNAs to the Treatment of Pancreatic Cancer Xenografts with FGFR and ALK Kinase Inhibitors. (PubMed, Cancers (Basel))
Mice with pancreatic cancer cell (COLO357PL) xenografts were treated with inhibitors of either fibroblast growth factor receptor kinase (FGFR; PD173074) or anaplastic lymphoma kinase receptor (ALK; TAE684)...Distinct signatures that include circulating miR-1 and miR-22 are associated with the efficacy of ALK and FGFR inhibition, respectively. We propose that monitoring changes in circulating miR profiles can provide an early signature of treatment response or resistance to pathway-targeted drugs, and thus provide a non-invasive measurement to rapidly assess the efficacy of candidate therapies.
Journal
|
ALK (Anaplastic lymphoma kinase) • FGFR (Fibroblast Growth Factor Receptor)
|
TAE-684
4years
Integrative analysis reveals clinically relevant molecular fingerprints in pancreatic cancer. (PubMed, Mol Ther Nucleic Acids)
Further integrative analysis revealed that temozolomide and NVP-TAE684 showed higher sensitivity in the C1 subgroup, whereas the C2 cell lines were more sensitive to SR1001 and SRT-1720. Our results also showed that PCCLs with mutations in CDKN2A, TP53, and SMAD4 were more sensitive to certain anti-cancer drugs. Our integrative analysis identified molecular features of pancreatic cancer that were associated with clinical significance and drug sensitivity, providing potentially effective strategies for precision treatments of patients with pancreatic cancer.
Clinical • Journal
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TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • SMAD4 (SMAD family member 4) • CD4 (CD4 Molecule)
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TP53 mutation • CDKN2A mutation • SMAD4 mutation
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temozolomide • TAE-684
over4years
Tumour-derived substrate-adherent cells promote neuroblastoma survival through secreted trophic factors. (PubMed, Mol Oncol)
In co-culture experiments, S-type cells protected N-type cells from apoptosis induced by the oncogenic ALK inhibitor TAE684...Overall, the tumour-derived S-type cells prevented apoptosis in the N-type cells via ALK-independent STAT3 activation triggered by secreted factors. The inhibition of these factors in combination with ALK inhibition could provide a new direction for targeted therapies to treat high-risk neuroblastoma.
Journal
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ALK (Anaplastic lymphoma kinase)
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ALK mutation
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TAE-684