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

Structure of compound 2

“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…

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