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

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 di...

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Veröffentlicht in:	EMBO reports 2024-09, Vol.25 (9), p.3944-3969
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Adaptor Proteins, Signal Transducing - genetics Adaptor Proteins, Signal Transducing - metabolism Animals Biomedical and Life Sciences Cell Line, Tumor Cell Proliferation - drug effects DNA-Binding Proteins - genetics DNA-Binding Proteins - metabolism Drug Resistance, Neoplasm - drug effects Drug Resistance, Neoplasm - genetics EMBO03 EMBO09 EMBO37 Gene Expression Regulation, Neoplastic - drug effects Hippo Signaling Pathway Humans Life Sciences Lipoylation Mice Mutation Protein Serine-Threonine Kinases - antagonists & inhibitors Protein Serine-Threonine Kinases - genetics Protein Serine-Threonine Kinases - metabolism Signal Transduction - drug effects Small Molecule Libraries - pharmacology TEA Domain Transcription Factors Transcription Factors - genetics Transcription Factors - metabolism Transcription, Genetic - drug effects Xenograft Model Antitumor Assays
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