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Comparative Assessment and High-Throughput Drug-Combination Profiling of TEAD-Palmitoylation Inhibitors in Hippo Pathway Deficient Mesothelioma

21 Nov 2023

Abstract excerpt

The hippo signaling pathway is a central tumor suppressor cascade frequently inactivated in selected human cancers, leading to the aberrant activation of TEAD transcription factors. Whereas several TEAD auto-palmitoylation inhibitors are currently in development, a comprehensive assessment of this novel drug-modality is missing. Here, we report a comparative analysis among six TEADi(s) using cell-based and...

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PMID: 38139762
DOI: 10.3390/ph16121635

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Related research

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Research trail→

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Comparative Assessment and High-Throughput Drug-Combination Profiling of TEAD-Palmitoylation Inhibitors in Hippo Pathway Deficient MesotheliomaPMID 38139762Read ↗

Identification of resistance mechanisms to small-molecule inhibition of TEAD-regulated transcription.Semantic proximity Read ↗

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

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

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

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

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

Palmitoylation landscapes across human cancers reveal a role of palmitoylation in tumorigenesisSemantic proximity Read ↗

Preclinical Characterization of Hippo pathway inhibition: Insights from Pharmacological and Genetic StudiesSemantic proximity Read ↗

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

P2.19-01 First-in-Human Phase 1 Trial of VT3989, a First-in-Class YAP/TEAD Inhibitor in Patients with Advanced MesotheliomaSemantic proximity Read ↗

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