vt104  (TargetMol)

Journal: Cancer Research Communications

Article Title: Aberrant Hippo-YAP/TEAD Signaling Drives Malignant Transcriptional Reprogramming in External Auditory Canal Squamous Cell Carcinoma

doi: 10.1158/2767-9764.CRC-25-0626

Figure Lengend Snippet: PITX2 acts as a potential partner TF of YAP in EACSCC. A and B, Dose–response curves of VT104 in ONO2 cells examined in a proliferation assay ( n = 6; A ) and a clonogenic assay ( n = 3; B ). C, qPCR for YAP/TAZ-TEAD target genes upon treatment with VT104 (1 μmol/L) for 24 hours in ONO2 cells in vitro ( n = 3). D, YAP Co-IP experiment in ONO2 cells treated with VT104 (1 μmol/L) for 24 hours. E, Dose–response curves of VT104 in ONO2 cells upon siRNA-mediated knockdown against PITX2 ( n = 6). The IC 50 value for each group is shown. F, Proliferation assays in ONO2 cells upon siRNA-mediated knockdown against PITX2 ( n = 3). G, Transwell migration assays in ONO2 and FaDu upon siRNA-mediated knockdown against PITX2 ( n = 5). H, A volcano plot representing DEGs between PITX2-overexpressed and control ONO2 cells. Selected genes are highlighted as yellow dots. Genes with an adjusted P value < 0.01 and an absolute value of fold change >1.5 were considered significant. I, GO analysis for the DEGs upregulated in PITX2-overexpressed ONO2 cells compared with control cells in the Molecular Signature Database (MSigDB) Hallmark pathways. J, GSEA representing gene sets positively or negatively enriched in PITX2-overexpressed ONO2 cells compared with control cells in MSigDB Hallmark pathways. K, Western blots for the indicated proteins in PITX2-overexpressed and control ONO2 cells. L, Proliferation assays in PITX2-overexpressed and control ONO2 cells ( n = 5). M, Wound healing assays in PITX2-overexpressed and control ONO2 cells ( n = 3). N, Spheroid formation assays in PITX2-overexpressed and control ONO2 cells ( n = 6). O and P, Growth curves for PITX2-overexpressed or control ONO2 xenograft tumors ( O ) and bar plots for tumor weight at endpoint ( P ; n = 6). The image of tumors is also shown. Q, Representative images for HE staining as well as immunohistochemical staining for PITX2 and Ki67 in the xenograft tumors. Data represent mean ± SEM. *, P < 0.05; **, P < 0.01; ***, P < 0.001; ****, P < 0.0001.

Article Snippet: Subsequently, cells were treated with VT104 TEAD inhibitor (#HY-134956, MedChemExpress) at concentrations ranging from 10 to 10,000 nmol/L for 6 days.

Techniques: Proliferation Assay, Clonogenic Assay, In Vitro, Co-Immunoprecipitation Assay, Knockdown, Migration, Control, Western Blot, Staining, Immunohistochemical staining

Journal: Cancer Research

Article Title: Oxytocin Receptor Regulates the Hippo/YAP Axis to Drive Hepatocarcinogenesis

doi: 10.1158/0008-5472.CAN-24-3405

Figure Lengend Snippet: YAP transcriptionally regulates OXTR expression, which forms a positive feedback loop between Hippo/YAP and the OXTR. A, OXTR expression was significantly correlated with that of CCN1 ( CYR61 ) and CCN2 ( CTGF ) in HCC samples from the TCGA database. B, OXTR genome schematic and database analysis of the binding region of YAP or TEAD to the OXTR. Sites 1‒4 CRISPRi sgRNAs were designed to target the four OXTR sites. C and D, YAP ChIP‒qPCR and qRT-qPCR with or without CRISPRi in YAP-overexpressing SNU449 cells. E‒G, qRT-qPCR indicated that siRNA, VP, or VT104 treatment via the indicated method in SNU449 cells decreased the CTGF and CYR61 mRNA levels. H‒J, Immunoblot analysis showing the expression level of the OXTR in SNU449 cells treated with siYAP, VP, or VT104 via the indicated methods. Treatment inhibited OXTR protein expression and mRNA expression. K‒M, RT-qPCR showing the mRNA expression levels of the OXTR with siYAP, VP, or VT104 treatment via the indicated method in SNU449 cells. N and O, Immunofluorescence imaging of the OXTR (red) and DAPI (blue) in SNU449 cells subjected to the indicated treatments. Scale bar, 10 μm. All data are presented as the means ± SDs. ns, nonsignificant; **, P < 0.01; ***, P < 0.001 for comparisons (Student t test).

Article Snippet: Atosiban (MedChemExpress, cat. #HY-17572), carbetocin (MedChemExpress, cat. #HY-17573), verteporfin (MedChemExpress, cat. #HY-B0146), GSK429286A (MedChemExpress, cat. #HY-11000), Y27632 (MedChemExpress, cat. #HY-10071), C3 (Cytoskeleton, cat. #CT03), and VT104 (MedChemExpress, cat. #HY-134956) are shown in Supplementary Table S3.

Techniques: Expressing, Binding Assay, Western Blot, Quantitative RT-PCR, Immunofluorescence, Imaging