Dissection of the interaction between the intrinsically disordered YAP protein and the transcription factor TEAD.
Elife
; 62017 04 21.
Article
em En
| MEDLINE
| ID: mdl-28430104
TEAD (TEA/ATTS domain) transcription factors are the most distal effectors of the Hippo pathway. YAP (Yes-associated protein) is a coactivator protein which, upon binding to TEAD proteins, stimulates their transcriptional activity. Since the Hippo pathway is deregulated in various cancers, designing inhibitors of the YAP:TEAD interaction is an attractive therapeutic strategy for oncology. Understanding the molecular events that take place at the YAP:TEAD interface is therefore important not only to devise drug discovery approaches, but also to gain knowledge on TEAD regulation. In this report, combining single site-directed mutagenesis and double mutant analyses, we conduct a detailed analysis on the role of several residues located at the YAP:TEAD interface. Our results provide quantitative understanding of the interactions taking place at the YAP:TEAD interface and give insights into the formation of the YAP:TEAD complex and more particularly on the interaction between TEAD and the Ω-loop found in YAP.
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MEDLINE
Assunto principal:
Fosfoproteínas
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Fatores de Transcrição
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Proteínas Adaptadoras de Transdução de Sinal
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Proteínas de Ligação a DNA
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Mapas de Interação de Proteínas
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Proteínas Musculares
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article