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TEA Domain Family Member (TEAD) Transcription Factors (TEAD)

Target
TEAD
Molecular classification
Transcription factor
01

Overview

The TEA domain family member (TEAD) transcription factors are a group of highly conserved proteins that play crucial roles in gene regulation, development, and disease. In humans, there are four main TEAD genes: TEAD1, TEAD2, TEAD3, and TEAD4. These proteins are characterized by the presence of a conserved DNA-binding region known as the "TEA domain". TEADs regulate genes controlling growth/development/apoptosis and are associated with cancer progression/proliferation/metastasis/stemness.

Other names
Transcriptional enhancer factor (TEF)TCF-13 (for TEAD1)
02

Mechanism of action

Small-molecule inhibitors targeting the palmitate-binding pocket within the C-terminal cofactor-interaction domain of mammalian TEADs disrupt auto-palmitoylation and block interaction with cofactors like YAP/TAZ.

03

Biological functions

Transcription regulationCell proliferationCell survivalCell differentiationOrgan developmentApoptosis regulationStemness maintenance
04

Disease associations

CancerChemoresistance
05

Safety considerations

Context-dependent oncogenic or tumor-suppressor activityAberrant Hippo pathway activity

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