Article

Discovery of a new class of reversible TEA-domain transcription factor inhibitors with a novel binding mode

2022-05-24

Abstract excerpt

<h4>ABSTRACT</h4> The TEA domain (TEAD) transcription factor forms a transcription co-activation complex with the key downstream effector of the Hippo pathway, YAP/TAZ. TEAD-YAP controls the expression of Hippo-responsive genes involved in cell proliferation, development, and tumorigenesis. Hyperactivation of TEAD-YAP activities is observed in many human cancers, and is associated with cancer cell proliferation,...

Topics

Open a Topic to create a Post that cites this publication.

Identifiers and source

Literature Corpus work: 168e3172-5a3a-53ba-9cb2-e7f7751db6b0
DOI: 10.1101/2022.05.24.493232

Open publication

Related research

Semantic proximity does not establish scientific evidence.

Click a neighbor to travelStep 1 · 12 closest

Discovery of a new class of reversible TEA-domain transcription factor inhibitors with a novel binding modeDOI 10.1101/2022.05.24.493232Read

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

Structure-based optimization of TEAD inhibitors: Exploring a novel subpocket near Glu347 for the treatment of NF2-mutant cancer.Semantic proximity Read

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

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

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

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

An improved TEAD dominant-negative protein inhibitor to study Hippo YAP1/TAZ-dependent transcriptionSemantic proximity Read

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

Targeting the Hippo pathway in cancers via ubiquitination dependent TEAD degradationSemantic proximity Read

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

TEAD is required for DNA repair independent of its transcriptional functionSemantic proximity Read

Dysregulation of the Hippo pathway enhances PD-L2 transcription to promote cancer immune evasionSemantic proximity Read