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Dissection of the interaction between the intrinsically disordered YAP protein and the transcription factor TEAD.


ABSTRACT: 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 ?-loop found in YAP.

SUBMITTER: Mesrouze Y 

PROVIDER: S-EPMC5400505 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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Dissection of the interaction between the intrinsically disordered YAP protein and the transcription factor TEAD.

Mesrouze Yannick Y   Bokhovchuk Fedir F   Meyerhofer Marco M   Fontana Patrizia P   Zimmermann Catherine C   Martin Typhaine T   Delaunay Clara C   Erdmann Dirk D   Schmelzle Tobias T   Chène Patrick P  

eLife 20170421


TEAD (<i>TEA</i>/ATTS <i>d</i>omain) transcription factors are the most distal effectors of the Hippo pathway. YAP (<i>Y</i>es-<i>a</i>ssociated <i>p</i>rotein) 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 interf  ...[more]

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