Small-Molecule Cyanamide Pan-TEAD·YAP1 Covalent Antagonists.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01189
Abstract: Transcriptional enhanced associate domains (TEADs) are transcription factors that bind to cotranscriptional activators like the yes-associated protein (YAP) or its paralog transcriptional coactivator with a PDZ-binding motif (TAZ). TEAD·YAP/TAZ target genes are involved in tissue… read more here.
Keywords: small molecule; cyanamide pan; pan tead; tead yap1 ... See more keywords
Abstract 7264: OPN-9840, a non-covalent potent pan-TEAD inhibitor, exhibits single agent efficacy in preclinical malignant mesothelioma models
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DOI: 10.1158/1538-7445.am2024-7264
Abstract: The Hippo pathway regulates critical cellular processes during development. In ~10% of human cancers, Hippo pathway dysregulation results in YAP/TAZ overactivation and increased TEAD-dependent transcription that promotes tumor growth and therapy resistance - often by… read more here.
Keywords: covalent; pan; pan tead; tead inhibitor ... See more keywords
Abstract 5362: Molecular profiling of SW-682, a pan-TEAD inhibitor, as monotherapy and in combination with other treatments across tumor types
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DOI: 10.1158/1538-7445.am2025-5362
Abstract: Hyperactivation of YAP/TAZ signaling (Hippo pathway) can drive oncogenesis across multiple cancer types by binding to the transcription factor TEAD and driving expression of target genes involved in cell proliferation and tumor progression. SW-682, an… read more here.
Keywords: cancer; combination; pan tead; tumor ... See more keywords