Data from: Basroparib inhibits YAP-driven cancers by stabilizing angiomotin
Data files
May 08, 2026 version files 231.25 KB
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Gene_set_data_analysis.xlsx
128.62 KB
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Processed_data_mRNA_level_J_reporter_gene_assay_J_IF_quantification_J_viability_data.xlsx
46.20 KB
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Quantification_data_WB.xlsx
30.61 KB
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Raw_data_Xenograft.xlsx
18.29 KB
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README.md
7.53 KB
Abstract
Yes‑associated protein (YAP) is a key oncogenic effector and a well‑established driver of resistance to anticancer therapies, especially in tumours harbouring KRAS mutations. Although YAP is clinically relevant, drug‑development efforts that directly inhibit its activity have been limited. Here, we show that basroparib—a selective tankyrase (TNKS) inhibitor that suppresses Wnt signalling—attenuates YAP‑driven oncogenic programmes by stabilising angiomotin (AMOT), an endogenous negative regulator of YAP. In colorectal cancer (CRC) cells, basroparib increased AMOT protein abundance, promoted AMOT–YAP complex formation, and enforced cytoplasmic sequestration of YAP, thereby dampening YAP‑dependent transcription. Basroparib preferentially sensitised YAP‑overexpressing, KRAS‑mutant CRC cell lines to MEK inhibition by disrupting the AMOT–YAP axis. In MEK inhibitor‑resistant CRC models, in which elevated YAP activity mediates escape, basroparib restored drug sensitivity both in vitro and in vivo. The compound also enhanced MEK inhibitor efficacy in other YAP‑active tumour types, while exerting minimal effects in YAP‑inactive models. Taken together, these results identify basroparib—now progressing through clinical development (Phase I, NCT04505839)—as a promising agent for dual Wnt–YAP pathway blockade and for overcoming therapeutic resistance in YAP‑driven cancers.
Dataset DOI: 10.5061/dryad.mkkwh71cx
Description of the data and file structure
Title
Basroparib, a Tankyrase-Wnt Pathway Inhibitor, Suppresses YAP-Driven Oncogenic Activity by Stabilizing Axin
Authors
Young-Ju Kwona,b†, Dong Young Kima†, Yuna Kima, Uk-Il Kimc, and Jae-Sung Kima,b*
aDivision of Radiation Biomedical Research, Korea Institute of Radiological and Medical Sciences, Seoul, Korea
bRadiological and Medico-Oncological Sciences, University of Science and Technology, Seoul, Korea
cST Pharm Co., Ltd., Seoul, Korea
†These authors contributed equally to this work.
Corresponding author: jaesung@kirams.re.kr
Data Overview
This dataset contains processed and quantified data supporting the findings of the manuscript titled "Basroparib, a Tankyrase–Wnt Pathway Inhibitor, Suppresses YAP-Driven Oncogenic Activity by Stabilizing Axin." The data provided are essential for validating the experimental results described in the manuscript.
Contents of the Dataset
1. Gene_set_data_analysis.xlsx
- Gene set enrichment and expression analysis related to YAP pathway activity.
- Includes:
• Analysis of YAP expression patterns across colorectal cancer cell line databases
• Correlation analyses of YAP1, TNKS1, and TNKS2 expression in colorectal, breast, lung, and pancreatic cancers
- Corresponds to Figures 7E and F
2.Processed_data_mRNA_level_J_reporter_gene_assay_J_IF_quantification_J_viability_data.xlsx
- Compiled processed datasets including:
• Quantitative PCR (qPCR) data (normalized gene expression values, fold changes, statistical significance)
• Reporter gene assay (luciferase activity)
• Immunofluorescence (IF) quantification (normalized intensity values)
• Cell viability assay data (dose–response and statistical analysis)
- Corresponds to Figures 1–7
3. Western Blot (WB) Quantification
- Quantified Western blot data showing relative protein expression
- Normalized to loading controls (e.g., β-actin)
- Corresponds to Figures 1–6
Usage Notes
All data are fully processed and ready for direct analysis.
Refer to the main manuscript for detailed experimental methods and interpretations.
Citation
If you use or reference this dataset in your research, please cite both the associated manuscript and this dataset in Dryad accordingly.
Files and variables
File: Gene_set_data_analysis1.xlsx
Description: Analysis of YAP expression patterns across colorectal cancer cell line databases and correlation analyses of YAP1, TNKS1, and TNKS2 expression in colorectal, breast, lung, and pancreatic cancers.
Transcript-level YAP1 expression data (TPM, pTPM, nTPM) across colorectal cancer cell lines (Fig. 3A)
Variables
Gene: Ensembl gene ID (e.g., ENSG00000137693)Gene.name: Gene symbol (e.g., YAP1)Cell.line: Cell line name (e.g., SW1417, OUMS-23)TPM: Transcripts per millionpTPM: Protein-coding TPMnTPM: Normalized TPM- Cross-cancer transcript expression analysis of YAP1, TNKS1, and TNKS2 across colorectal, breast, lung, and pancreatic cancer types.
- Variables:
Cancer_Type: Colorectal, Breast, Lung, Pancreatic (inferred from column grouping)YAP1: Transcript expression level of YAP1TNKS1: Transcript expression level of TNKS1TNKS2: Transcript expression level of TNKS2
File: Processed_data_mRNA_level__reporter_gene_assay__IF_quantification__viability_data.xlsx
Description: This file contains normalized and processed experimental data from multiple assays, including mRNA expression (qPCR), reporter gene assays (e.g., luciferase), immunofluorescence (IF) quantification, and cell viability measurements under various treatment conditions (e.g., Basroparib, control, combination therapy).
Variables
- [mRNA Expression]
Cell_Line: Name of the cell line (e.g., SW480, DLD1)Gene: Target gene measured (e.g., CTGF, CYR61, AXIN2)Drug_Concentration: Basroparib or compound concentration in μMRelative_Expression: Normalized gene expression level (often relative to vehicle-treated control)
[Reporter Gene Assay]Reporter_Type: Type of luciferase or reporter construct (e.g., 8xGTIIC-Luc, TEAD-activity reporter)Treatment_Group: Drug or combination used (e.g., Basroparib)Luciferase_Activity: Normalized luciferase output (e.g., fold-change relative to control)Replicate: Biological replicate number
[IF Quantification]Target_Protein: Marker visualized by IF (e.g., YAP)Fluorescence_Intensity: Quantified intensity value per cell or per imageTreatment_Condition: Drug treatment group
[Cell Viability]Cell_Line: Cell line nameDrug: Name of drug administered (e.g., Basroparib)Concentration: μMViability_%: Cell viability expressed as percentage relative to control
File: Quantification_data_WB.xlsx
Description: Quantified Western blot data showing relative expression levels of key signaling proteins across various treatment conditions and cell lines.
Variables
Protein_Name: Protein measured in each blot (e.g., YAP, AMOT, CTGF)Cell_Line: Name of the cell line analyzed (e.g., SW480, DLD-1)Drug_Concentration: Concentration of Basroparib treatment (e.g., 0, 5, 10 μM)Relative_Band_Intensity: Quantified signal intensity of target protein normalized to loading control (e.g., β-actin)Replicate: Experimental replicate numberTreatment_Group: Experimental condition (e.g., DMSO, Basroparib, combo)Blot_ID: Reference to the figure panel or blot (e.g., Fig.1C, Fig.2A)
File: Raw_data_Xenograft.xlsx
Description: Raw xenograft data including tumor volume measurements and experimental conditions in xenograft mouse models.
- Variables:
Day: Number of days since treatment initiation or tumor implantation (e.g., 0, 4, 7, 11, …)Treatment_Group: Experimental groups including Vehicle, Basroparib (Bas), Combination therapy (Combo)Mouse_ID: Individual columns representing each mouse within each treatment group (implicitly labeled)Tumor_Volume_mm3: Tumor size at each time point, measured in cubic millimeters (mm³)
Code/software
All data files were created and processed using Microsoft Excel. No custom code or scripts were used to generate or analyze the data in this submission. All values have been pre-processed and manually curated in Excel to ensure compatibility across spreadsheet platforms. No additional software or packages are required.
Access information
Other publicly accessible locations of the data:
- None.
Data was derived from the following sources:
- The Human Protein Atlas
- Website: https://www.proteinatlas.org
- Description: RNA-seq expression data for colorectal cancer (CRC) were obtained for correlation analysis.
- License: Open-access for academic use, as per HPA terms of use.
- The Cancer Genome Atlas (TCGA) via cBioPortal
- Website: https://www.cbioportal.org
- Description: Gene expression data for colorectal, breast, lung, and pancreatic cancer patient samples were accessed through the Genomic Data Commons via cBioPortal.
- License: Open-access under the NIH Genomic Data Sharing (GDS) policy.
