GEO series

Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in Hippo-dependent cancer models [Quant-seq]

GSE305227 Homo sapiens (human) RNA-seq (gene expression) 149 samples Submitted 2026/05/07 Platform GPL16791

At a glance

RNA-seq (gene expression) · human · 149 samples

What it is: RNA-seq (gene expression)Gene activity measured by sequencing. The summary does not mention single-cell work, so this is most likely bulk: one average per sample, the usual starting point for comparing groups.
Organism: Homo sapiens (human)
Samples: 149 samples: 120 distinct titles, 10 of them repeatedGroups are read from the sample names, not from the paper. Check the list below.
Data you can get: A processed table (series matrix) and supplementary files from NCBI; the raw sequencing reads from ENA. Which of these hold counts depends on the study, so check the file list.

Summary (written by the submitters)

TEAD proteins are a family of transcription factors that enable the oncogenic activity of deregulated Hippo signaling and are a promising therapeutic target in oncology. Targeting the lipid pocket of TEAD is an established path to inhibit the oncogenic activities of the cofactors YAP and TAZ. Here we present two covalent pan-TEAD inhibitors that bind to the lipid pocket, GNE-8025 and GNE-2181.

Read the full summary ↓

GNE-8025 binds TEAD proteins covalently at a conserved cysteine residue to engage the lipid pocket and allosterically disrupt the interaction of TEAD proteins with YAP. GNE-2181 is a further optimized version of GNE-8025 with properties that enable brain penetrance in vivo. Both of these small molecules suppress the proliferation of YAP-driven tumor cells both in vitro and in vivo and increase activity of a broad range of inhibitors of the MAPK pathway. We demonstrate that these molecules have exceptional efficacy in Hippo-driven in vivo tumor models, including in a mouse model of brain metastases where GNE-2181 treatment significantly inhibits the growth of intracranial brain tumors. Altogether we present a next-generation class of TEAD inhibitors. The development of GNE-8025 and GNE-2181 is a significant advancement towards potent, specific, and effective Hippo-targeting cancer therapies.

This dataset

Open GSE305227 in finder → Find more human RNA-seq datasets →

Download · which file do I need?

Direct links to NCBI and ENA, no account and no request form. Pick by what you want to do: take the small processed table to look, the supplementary files to re-analyse, or the original raw data to start over.

1 · Just have a look

Processed table

The series matrix: one table of values per sample as the submitters processed it. The smallest download, and it opens in Excel or R. Start here to see what the data look like.

Series matrix ↓

2 · Re-analyse it

Supplementary files

The count tables and other files the authors uploaded. Take only the samples you need, or the whole study as GSE305227_RAW.tar (it can run to tens of gigabytes).

All supplementary files ↗ Whole study · RAW.tar ↓

3 · Start from the raw reads

Raw sequencing reads

The original FASTQ files, straight from the sequencer, held at ENA. Large, and you align them yourself, so only choose this if you need to re-process the study from scratch.

Raw reads on ENA ↗

What the files usually look like: For RNA-seq the counts are usually a table among the supplementary files (look for 'counts', 'expression', 'FPKM' or 'TPM' in the file name). The series matrix of a sequencing study is sometimes nearly empty.

Also filed as BioProject PRJNA1304868. Searching any of these in the dataset finder brings you back here.

NCBI GEO page ↗

Study design

120 distinct titles, 10 of them repeated

NGS4532 BP043209 ES-2 DMSO, ×8 NGS4532 BP043210 NCI-H226 DMSO, ×4 NGS4532 BP045307 NCI-H226 DMSO, ×4 NGS4532 BP045308 NCI-H226 DMSO, ×4 NGS4532 BP045309 ES-2 DMSO, ×4 NGS4532 BP045309 NCI-H358 DMSO, ×4 NGS4532 BP043210 NCI-H358 DMSO, ×3 NGS4532 BP045307 NCI-H358 DMSO, ×3 +2 more

How we read this: Read from 149 sample titles: 120 distinct titles with little repetition. These groups are guessed from the sample names, not taken from the paper, so check them against the sample list below before relying on them.

Samples in this study

GSM9165871 NGS4532 BP043209 ES-2 G03502181, Replicate 1
GSM9165872 NGS4532 BP043209 ES-2 DMSO, Replicate 1
GSM9165873 NGS4532 BP043209 ES-2 DMSO, Replicate 2
GSM9165874 NGS4532 BP043209 ES-2 DMSO, Replicate 3
GSM9165875 NGS4532 BP043209 ES-2 DMSO, Replicate 4
GSM9165876 NGS4532 BP043209 ES-2 G03502181, Replicate 2
GSM9165877 NGS4532 BP043209 ES-2 DMSO, Replicate 5
GSM9165878 NGS4532 BP043209 ES-2 DMSO, Replicate 6
GSM9165879 NGS4532 BP043209 ES-2 DMSO, Replicate 7
GSM9165880 NGS4532 BP043209 ES-2 DMSO, Replicate 8
GSM9165881 NGS4532 BP043210 NCI-H226 G03502181, Replicate 1
GSM9165882 NGS4532 BP043210 NCI-H226 DMSO, Replicate 1
GSM9165883 NGS4532 BP043210 NCI-H226 DMSO, Replicate 2
GSM9165884 NGS4532 BP043210 NCI-H226 DMSO, Replicate 3
GSM9165885 NGS4532 BP043210 NCI-H226 DMSO, Replicate 4
GSM9165886 NGS4532 BP043210 NCI-H358 G03502181, Replicate 2
GSM9165887 NGS4532 BP043210 NCI-H358 DMSO, Replicate 5
GSM9165888 NGS4532 BP043210 NCI-H358 DMSO, Replicate 6
GSM9165889 NGS4532 BP043210 NCI-H358 DMSO, Replicate 7
GSM9165890 NGS4532 BP045307 NCI-H226 G03502181, Replicate 1
GSM9165891 NGS4532 BP045307 NCI-H226 DMSO, Replicate 1
GSM9165892 NGS4532 BP045307 NCI-H226 DMSO, Replicate 2
GSM9165893 NGS4532 BP045307 NCI-H226 DMSO, Replicate 3
GSM9165894 NGS4532 BP045307 NCI-H226 DMSO, Replicate 4
GSM9165895 NGS4532 BP045307 NCI-H358 G03502181, Replicate 2
GSM9165896 NGS4532 BP045307 NCI-H358 DMSO, Replicate 5
GSM9165897 NGS4532 BP045307 NCI-H358 DMSO, Replicate 6
GSM9165898 NGS4532 BP045307 NCI-H358 DMSO, Replicate 7
GSM9165899 NGS4532 BP045308 NCI-H226 G03502181, Replicate 1
GSM9165900 NGS4532 BP045308 NCI-H226 DMSO, Replicate 1
GSM9165901 NGS4532 BP045308 NCI-H226 DMSO, Replicate 2
GSM9165902 NGS4532 BP045308 NCI-H226 DMSO, Replicate 3
GSM9165903 NGS4532 BP045308 NCI-H226 DMSO, Replicate 4
GSM9165904 NGS4532 BP045308 NCI-H358 G03502181, Replicate 2
GSM9165905 NGS4532 BP045308 NCI-H358 DMSO, Replicate 5
GSM9165906 NGS4532 BP045308 NCI-H358 DMSO, Replicate 6
GSM9165907 NGS4532 BP045308 NCI-H358 DMSO, Replicate 7
GSM9165908 NGS4532 BP045309 ES-2 G03502181, Replicate 1
GSM9165909 NGS4532 BP045309 ES-2 DMSO, Replicate 1
GSM9165910 NGS4532 BP045309 ES-2 DMSO, Replicate 2

+ 109 more — browse all 149 samples with per-sample file links →

Datasets on a similar topic

GSE305224 Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in Hippo-dependent cancer models [RNA-seq] 120 samples shares yap, hippo-dependent, demonstrate, inhibitors, penetrance, covalent, pan-tead
GSE305254 Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in Hippo-dependent cancer models 299 samples shares yap, hippo-dependent, demonstrate, inhibitors, penetrance, covalent, pan-tead
GSE330305 Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in Hippo-dependent cancer models [ATAC-seq] 30 samples shares yap, hippo-dependent, demonstrate, inhibitors, penetrance, covalent, pan-tead
GSE229195 Synergism of FAK and ROS1 inhibitors in the treatment of CDH1-deficient cancers mediated by FAK-YAP-TRX signaling 12 samples shares yap, inhibitors
GSE313416 Transient proliferation by reversible YAP- and mitogen-control of the cyclin D1/p27 ratio 63 samples shares yap
GSE318597 Physiological perfusion of human vasculature reveals a YAP/TAZ-Apelin switch linking intraluminal flow to endothelial state transitions and vessel remodeling 34 samples shares yap
GSE318595 Physiological perfusion of human vasculature reveals a YAP/TAZ-Apelin switch linking intraluminal flow to endothelial state transitions and vessel remodeling [Bulk RNA-seq] 31 samples shares yap
GSE333379 AXL phosphosite mapping links FAK1 and YAP1 signaling to erlotinib resistance in EGFR-mutant lung cancer 29 samples shares yap

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Metadata from NCBI GEO, cached and refreshed periodically — the NCBI page above is authoritative. Downloads link straight to NCBI/ENA; nothing is proxied through BioTransfer.