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Article

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

Bioorganic chemistry - 1 Jun 2025

Kim Jin Kwan, Kim Jinhyuk, Kim Hadong, Jin Haiyan, Yoo Youngki, Fei Xiang, Maeng Han-Joo, Seo Seung-Yong, Han Gyoonhee, No Kyoung Tai

Abstract excerpt

The Hippo signaling pathway is critical for regulating cell growth, tissue homeostasis, and organ size. Dysregulation of this pathway has been associated with a range of pathologies, especially cancer, through its modulation of downstream effectors-Yes-associated protein (YAP) and the transcriptional coactivator with PDZ-binding motif (TAZ). These proteins bind to transcriptional enhanced associate domain (TEAD)...

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Identifiers

PMID: 40168885
DOI: 10.1016/j.bioorg.2025.108425

Genes

NF2
TEAD3

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 8 Sept 2026.

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Structure-based optimization of TEAD inhibitors: Exploring a novel subpocket near Glu347 for the treatment of NF2-mutant cancer.PMID 40168885Read ↗

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

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

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