^
7d
Discovery of key molecular signatures for diagnosis and therapies of glioblastoma by combining supervised and unsupervised learning approaches. (PubMed, Sci Rep)
Finally, we recommended KGs-guided four repurposable drug molecules (Fluoxetine, Vatalanib, TGX221 and RO3306) against GBM through molecular docking, drug likeness, ADMET analyses and molecular dynamics simulation studies. Thus, the discoveries of this study could serve as valuable resources for wet-lab experiments in order to take a proper treatment plan against GBM.
Journal
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TOP2A (DNA topoisomerase 2-alpha) • RAD51 (RAD51 Homolog A) • AURKA (Aurora kinase A) • CHEK1 (Checkpoint kinase 1) • RAD51AP1 (RAD51 Associated Protein 1) • CCNB2 (Cyclin B2) • CDK1 (Cyclin-dependent kinase 1) • MCM10 (Minichromosome Maintenance 10 Replication Initiation Factor) • CDCA8 (Cell Division Cycle Associated 8)
|
TGX-221 • fluoxetine • vatalanib (PTK787)
9ms
SP1 Mediated PIK3CB Upregulation Promotes Gastric Carcinogenesis. (PubMed, J Cancer)
TGX-221, a PIK3CB-selective inhibitor, which can block this signaling transduction pathway, was found to inhibit the growth of GC cells and induce apoptosis in vitro, implying that it may act as a potential development agent for GC. These collective findings provide a new insight into PI3K/AKT signaling that SP1 may function as an upstream factor on PI3K, forming a new signaling axis to promote the progression of GC or other malignancies.
Journal
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PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
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TGX-221
10ms
Bioinformatics analysis identifies coagulation factor II receptor as a potential biomarker in stomach adenocarcinoma. (PubMed, Sci Rep)
Drug sensitivity analysis demonstrated positive correlations between F2R and several drugs, including BEZ235, CGP-60474, Dasatinib, HG-6-64-1, Aazopanib, Rapamycin, Sunitinib and TGX221, while negative correlation with CP724714, FH535, GSK1904529A, JNK-9L, LY317615, pyrimidine, rTRAIL and Vinorelbine. In conclusion, this study underscores the significance of F2R as a potential biomarker in gastric adenocarcinoma, shedding light on its molecular mechanisms in tumorigenesis. F2R holds promise for aiding in the diagnosis, prognosis, and targeted therapy of STAD.
Journal
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TGFB1 (Transforming Growth Factor Beta 1)
|
dasatinib • sunitinib • dactolisib (RTB101) • vinorelbine tartrate • sirolimus • Kinenza (enzastaurin) • TGX-221
over1year
Advances in lung adenocarcinoma: A novel perspective on prognoses and immune responses of CENPO as an oncogenic superenhancer. (PubMed, Transl Oncol)
CENPO was found to be positively associated with the expression levels of immune checkpoints and drug IC50 value (Roscovitine and TGX221), but negatively associated with the fraction levels of several immature cells and drug IC50 value (CCT018159, GSK1904529A, Lenaildomide, and PD-173074). The removal of CENPO significantly suppressed metastasis and induced arrest and apoptosis of LUAD cells. The involvement of CENPO in the immunosuppression of LUAD provides a prognostic signature for LUAD patients.
Journal
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TGX-221 • seliciclib (CYC202)
over1year
Glucose 6 phosphatase dehydrogenase (G6PD): a novel diagnosis marker related to gastrointestinal cancers. (PubMed, Am J Transl Res)
G6PD is highly expressed in gastrointestinal cancers. It is a carcinogenic indicator related to prognosis and can be used as a potential diagnostic marker of gastrointestinal cancers, so as to provide new strategy for cancer treatment.
Journal
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TP53 (Tumor protein P53) • CD276 (CD276 Molecule) • CD4 (CD4 Molecule) • HHLA2 (HERV-H LTR-Associating 2) • G6PD (Glucose-6-Phosphate Dehydrogenase) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase)
|
TP53 mutation
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daunorubicin • daporinad (APO866) • TGX-221
over1year
Probing the Potential of Defense Response-Associated Genes for Predicting the Progression, Prognosis, and Immune Microenvironment of Osteosarcoma. (PubMed, Cancers (Basel))
This study elucidated the role and mechanism of BNIP3, PTGIS, and ZYX in OS progression and was well verified by the experimental results, enabling reliable prognostic means and treatment strategies to be proposed for OS patients.
Journal
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CD8 (cluster of differentiation 8)
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TGX-221 • amuvatinib (MP470)
over1year
Uses of Vascular Endothelial Growth Factor C as a Lung Adenocarcinoma Prognostic Biomarker. (PubMed, World J Oncol)
The sensitivity of 5-fluorouracil was positively correlated with VEGF-C, and the sensitivity of TGX221 was negatively correlated with VEGF-C. The activity of BI-2536 and BRD-A94377914 was positively correlated with VEGF-C. Novel LUAD prognostic biomarkers such as VEGF-C mRNA may aid diagnosis and treatment, and may help identify optimal LUAD populations for therapeutic treatments.
Journal
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EGFR (Epidermal growth factor receptor) • TP53 (Tumor protein P53) • NF1 (Neurofibromin 1) • VEGFA (Vascular endothelial growth factor A) • CD4 (CD4 Molecule) • VEGFC (Vascular Endothelial Growth Factor C)
|
TP53 mutation • NF1 mutation • TP53 expression • VEGFA expression
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5-fluorouracil • BI2536 • TGX-221
2years
Study on the prognosis, immune and drug resistance of m6A-related genes in lung cancer. (PubMed, BMC Bioinformatics)
In conclusion, m6A-related genes are important participants in LC and the expression levels of ZC3H13, CBLL1, ELAVL1 and YTHDF1 are significant for prediction and treatment of LC. Researches of drug resistance based on m6A-related genes need to pay more attention for producing new therapeutic strategies of LC and CBLL1 may contribute to target treatment for further research.
Journal
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CD4 (CD4 Molecule) • ELAVL1 (ELAV Like RNA Binding Protein 1) • HNRNPC (Heterogeneous Nuclear Ribonucleoprotein C) • YTHDF2 (YTH N6-Methyladenosine RNA Binding Protein 2)
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Xalkori (crizotinib) • erlotinib • Gilotrif (afatinib) • dasatinib • lapatinib • etoposide IV • TGX-221
over2years
Circular dorsal ruffles disturb the growth factor-induced PI3K-AKT pathway in hepatocellular carcinoma Hep3B cells. (PubMed, Cell Commun Signal)
Our results showed that CDRs modulate the AKT pathway in Hep3B cells. Since CDRs were not observed in other HCC and hepatocyte cell lines, we propose that CDRs in Hep3B would determine the carcinoma characteristic of the cell by aberrantly triggering the AKT pathway. Signaling molecules involved in CDR formation are promising therapeutic targets for some types of HCC. Video abstract.
Journal
|
EGF (Epidermal growth factor)
|
TGX-221
over2years
SAA1 Expression as a Potential Prognostic Marker of the Tumor Microenvironment in Glioblastoma. (PubMed, Front Neurol)
The altered expression level shifts the primary function of SAA1 from cell cycle and mitosis to immune activity. High expression of SAA1 is associated with poor survival and upregulates the expression of LAIR1 and TNFSF14, thereby deeming it as the drug sensitivity indicator for XAV939, TGX-221, and lapatinib in GBM immune therapy.
Journal • Tumor Mutational Burden
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TMB (Tumor Mutational Burden) • SAA1 (Serum Amyloid A1) • LAIR1 (Leukocyte Associated Immunoglobulin Like Receptor 1) • TNFSF14 (TNF Superfamily Member 14)
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LAIR1 expression
|
lapatinib • TGX-221 • XAV-939
over2years
Combined Treatment with PI3K Inhibitors BYL-719 and CAL-101 Is a Promising Antiproliferative Strategy in Human Rhabdomyosarcoma Cells. (PubMed, Molecules)
In the study reported here, a panel of five compounds targeting the catalytic subunits of the four class I PI3K isoforms (p110α, BYL-719 inhibitor; p110β, TGX-221 inhibitor; p110γ, CZC24832; p110δ, CAL-101 inhibitor) and the dual p110α/p110δ, AZD8835 inhibitor, were tested on the RMS cell lines RD, A204, and SJCRH30. When combined with CAL-101, BYL-719 decreased cell viability and induced apoptosis in a synergistic manner, equaling or surpassing results achieved with AZD8835. In conclusion, our findings indicate that BYL-719, either alone or in combination with the p110δ inhibitor, CAL-101, could represent an efficient treatment for human rhabdomyosarcoma presenting with aberrant upregulation of the PI3K signaling pathway.
Journal
|
PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma)
|
Piqray (alpelisib) • Zydelig (idelalisib) • AZD8835 • CZC24832 • TGX-221
over2years
Identification and Characterization of a Glucometabolic Prognostic Gene Signature in Neuroblastoma based on N6-methyladenosine Eraser ALKBH5. (PubMed, J Cancer)
TGX-221 was predicted to be a potential therapeutic drug and validated to suppress NB oncogenes including MYCN, AHCY and NCAN and immunosuppressive DNMT1 in NB cells. ALKBH5 was closely related to glucometabolic processes, and our prognostic model had high application value in predicting & assessing the OS of NB patients, and even served potential drug targets.
Journal • Gene Signature
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MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • DNMT1 (DNA methyltransferase 1) • AKR1C2 (Aldo-Keto Reductase Family 1 Member C2) • ALKBH5 (AlkB Homolog 5, RNA Demethylase)
|
TGX-221
over2years
Integrative Analysis for Identification of Therapeutic Targets and Prognostic Signatures in Non-Small Cell Lung Cancer. (PubMed, Bioinform Biol Insights)
On the contrary, high mRNA expressions of CBL, FYN, LRKK2, and SOCS2 were associated with a significantly better prognosis. Furthermore, our drug target analysis for these hub genes suggests a potential use of Trichostatin A, Pracinostat, TGX-221, PHA-793887, AG-879, and IMD0354 antineoplastic agents to reverse the expression of these DEGs in NSCLC patients.
Journal
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • EZH2 (Enhancer of zeste 2 polycomb repressive complex 2 subunit) • AURKA (Aurora kinase A) • CDC20 (Cell Division Cycle 20) • CDK1 (Cyclin-dependent kinase 1) • SOCS2 (Suppressor Of Cytokine Signaling 2) • FYN (FYN Proto-Oncogene, Src Family Tyrosine Kinase)
|
AURKA overexpression
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pracinostat (SB939) • PHA 793887 • TGX-221
over2years
Context dependent isoform specific PI3K inhibition confers drug resistance in hepatocellular carcinoma cells. (PubMed, BMC Cancer)
Simultaneously constructed and analyzed differentially expressed cellular networks presented in this study, revealed distinct consequences of isoform specific PI3K inhibition in PTEN adequate and deficient liver cancer cells. We demonstrated the importance of context dependent and isoform specific PI3K/Akt/mTOR signaling inhibition in drug resistance during combination therapies. ( https://github.com/cansyl/Isoform-spesific-PI3K-inhibitor-analysis ).
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
|
sorafenib • TGX-221 • PIK-75
almost3years
Connexin 43 confers chemoresistance through activating PI3K. (PubMed, Oncogenesis)
To explore the therapeutic potential of simultaneously targeting Cx43 and PIK3CB/p110β, αCT1 is combined with TGX-221 or GSK2636771, two PIK3CB/p110β-selective inhibitors. These two different treatments synergistically inactivate PI3K and sensitize glioblastoma cells to temozolomide in vitro and in vivo. Our study has revealed novel mechanistic insights into Cx43/PI3K-mediated temozolomide resistance in glioblastoma and demonstrated that targeting Cx43 and PIK3CB/p110β together is an effective therapeutic approach for overcoming chemoresistance.
Journal
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PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta) • PI3K (Phosphoinositide 3-kinases)
|
temozolomide • GSK2636771 • TGX-221
3years
Phosphoproteomics identifies PI3K inhibitor-selective adaptive responses in pancreatic cancer cell therapy and resistance. (PubMed, Mol Cancer Ther)
We compared the effects of LY294002 that inhibit with equal potency all class I isoenzymes and downstream mTOR with the action of inhibitors with higher isoform-selectivity towards PI3Kα, PI3Kβ or PI3Kγ (namely A66, TGX-221 and AS-252424). The combination of clinically approved a-selective BYL-719 with γ-selective IPI-549 was more efficient than single molecule treatment on xenograft growth. Mapping unique adaptive signaling responses to isoform-selective PI3K inhibition will help to design better combinative treatments that prevent the induction of selective compensatory signals.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PIK3CG (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Gamma) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
|
Piqray (alpelisib) • LY294002 • eganelisib (IPI-549) • TGX-221
almost4years
Predicting Non-Alcoholic Fatty Liver Disease Progression and Immune Deregulations by Specific Gene Expression Patterns. (PubMed, Front Immunol)
Meanwhile, AKR1B10 and SPP1 are closely related to the above three immune cell infiltrations and immunosuppressive cytokines expressions in NAFLD and NAFLD-HCC. Subsequently, we screened out AKR1B10 and SPP1 sensitive molecules TGX-221, which may provide a possible therapy for NAFLD and NAFLD-HCC.
Journal
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SPP1 (Secreted Phosphoprotein 1)
|
TGX-221