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Article

Identification of resistance mechanisms to small-molecule inhibition of TEAD-regulated transcription.

EMBO reports - 1 Sept 2024

Kulkarni Aishwarya, Mohan Varshini, Tang Tracy T, Post Leonard, Chan Yih-Chih, Manning Murray, Thio Niko, Parker Benjamin L, Dawson Mark A, Rosenbluh Joseph, Vissers Joseph Ha, Harvey Kieran F

Abstract excerpt

The Hippo tumor suppressor pathway controls transcription by regulating nuclear abundance of YAP and TAZ, which activate transcription with the TEAD1-TEAD4 DNA-binding proteins. Recently, several small-molecule inhibitors of YAP and TEADs have been reported, with some entering clinical trials for different cancers with Hippo pathway deregulation, most notably, mesothelioma. Using genome-wide CRISPR/Cas9 screens...

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Topics

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Share to Adaptor Proteins, Signal Transducing
Share to Drug Resistance, Neoplasm

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Gene Expression Regulation, Neoplastic

Share to Hippo Signaling Pathway

Share to Lipoylation

Share to Protein Serine-Threonine Kinases

Share to Small Molecule Libraries

Share to Xenograft Model Antitumor Assays

Source

Open in PubMed Open full text

Identifiers

PMID: 39103676
DOI: 10.1038/s44319-024-00217-3
PMCID: PMC11387499

Genes

TEAD1
TEAD4

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

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Research trail→

Click a neighbor to travelStep 1 · 12 closest

Identification of resistance mechanisms to small-molecule inhibition of TEAD-regulated transcription.PMID 39103676Read ↗

Identification of resistance mechanisms to small-molecule inhibition of TEAD-regulated transcriptionSemantic proximity Read ↗

A Novel Irreversible TEAD Inhibitor, SWTX-143, Blocks Hippo Pathway Transcriptional Output and Causes Tumor Regression in Preclinical Mesothelioma ModelsSemantic proximity Read ↗

Comparative Assessment and High-Throughput Drug-Combination Profiling of TEAD-Palmitoylation Inhibitors in Hippo Pathway Deficient MesotheliomaSemantic proximity Read ↗

Structure-based discovery of a novel small-molecule inhibitor of TEAD palmitoylation with anticancer activitySemantic proximity Read ↗

Pipeline to evaluate YAP-TEAD inhibitors indicates TEAD inhibition represses NF2-mutant mesothelioma.Semantic proximity Read ↗

Direct and selective pharmacological disruption of the YAP–TEAD interface by IAG933 inhibits Hippo-dependent and RAS–MAPK-altered cancersSemantic proximity Read ↗

Statin suppresses Hippo pathway-inactivated malignant mesothelioma cells and blocks the YAP/CD44 growth stimulatory axis.Semantic proximity Read ↗

Development of a pipeline to evaluate YAP-TEAD inhibitor potential <i>-</i> direct TEAD inhibition represses cancerous growth in a <i>NF2</i> -mutant model of mesotheliomaSemantic proximity Read ↗

Discovery of a new class of reversible TEA-domain transcription factor inhibitors with a novel binding modeSemantic proximity Read ↗

Targeted degradation of specific TEAD paralogs by small molecule degradersSemantic proximity Read ↗

CRISPR Screening Identifies WEE1 as a Combination Target for Standard Chemotherapy in Malignant Pleural MesotheliomaSemantic proximity Read ↗

Genetic screens reveal new targetable vulnerabilities in BAP1-deficient mesotheliomaSemantic proximity Read ↗

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