Structure of 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

“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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