Targeting the YAP-TEAD interaction interface for therapeutic intervention in glioblastoma.

ABSTRACT:

Introduction

Recent studies have suggested that dysregulated Hippo pathway signaling may contribute to glioblastoma proliferation and invasive characteristics. The downstream effector of the pathway, the Yes-associated protein (YAP) oncoprotein, has emerged as a promising target in glioblastoma multiforme (GBM).

Methods

Utilizing a high-throughput yeast two-hybrid based screen, a small molecule was identified which inhibits the association of the co-transcriptional activator YAP1 and the TEA domain family member 1 (TEAD1) transcription factor protein-protein interaction interface. This candidate inhibitor, NSC682769, a novel benzazepine compound, was evaluated for its ability to affect Hippo/YAP axis signaling and potential anti-glioblastoma properties.

Results

NSC682

SUBMITTER: Saunders JT 

PROVIDER: S-EPMC8005474 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature