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Sep. 18, 2021

Compound 2: A TEAD Transcription Factor Lipidation Modulator

"Compound 2"

TEAD transcription factor lipidation modulator orally active in xenograft model from 1M cmpd biochemical HTS and opt. Cell Reports, Jun. 23, 2020 Genentech, South San Francisco, CA

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Drug Hunter Team

“Compound 2” binds to a lipid pocket on TEAD transcription factors, transforming TEAD from a transcriptional co-activator to a dominant-negative transcriptional repressor of Hippo pathway signaling. The tool molecule demonstrates activity against xenograft models, and will be useful for understanding Hippo pathway biology.

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