4LN0

Crystal structure of the VGLL4-TEAD4 complex

4LN0 の概要

• エントリーDOI: 10.2210/pdb4ln0/pdb
• 分子名称: Transcriptional enhancer factor TEF-3, Transcription cofactor vestigial-like protein 4, DI(HYDROXYETHYL)ETHER, ... (5 entities in total)
• 機能のキーワード: tea/atts domain family, vestigial/tondu family, transcription factor, transcription cofactor, development, transcription
• 由来する生物種: Mus musculus (mouse); 詳細
• 細胞内の位置: Nucleus: Q62296; Nucleus (By similarity): Q80V24
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 58678.17

構造登録者

Wang, H.,Shi, Z.,Zhou, Z. (登録日: 2013-07-11, 公開日: 2014-02-26, 最終更新日: 2023-11-08)

主引用文献

Jiao, S.,Wang, H.,Shi, Z.,Dong, A.,Zhang, W.,Song, X.,He, F.,Wang, Y.,Zhang, Z.,Wang, W.,Wang, X.,Guo, T.,Li, P.,Zhao, Y.,Ji, H.,Zhang, L.,Zhou, Z.
A Peptide Mimicking VGLL4 Function Acts as a YAP Antagonist Therapy against Gastric Cancer.
Cancer Cell, 25:166-180, 2014

PubMed Abstract: The Hippo pathway has been implicated in suppressing tissue overgrowth and tumor formation by restricting the oncogenic activity of YAP. However, transcriptional regulators that inhibit YAP activity have not been well studied. Here, we uncover clinical importance for VGLL4 in gastric cancer suppression and find that VGLL4 directly competes with YAP for binding TEADs. Importantly, VGLL4's tandem Tondu domains are not only essential but also sufficient for its inhibitory activity toward YAP. A peptide mimicking this function of VGLL4 potently suppressed tumor growth in vitro and in vivo. These findings suggest that disruption of YAP-TEADs interaction by a VGLL4-mimicking peptide may be a promising therapeutic strategy against YAP-driven human cancers.

PubMed: 24525233
DOI: 10.1016/j.ccr.2014.01.010

実験手法

X-RAY DIFFRACTION (2.896 Å)