Grainyhead-like transcription factor 3 (GRHL3)

Grainyhead-like transcription factor 3 (GRHL3) is a member of the highly conserved grainyhead transcription factor family, functioning as a DNA-binding transcription factor with a crucial role in multiple developmental processes, especially the differentiation and maintenance of stratified epithelial tissues. It directly binds distinct cis-regulatory DNA elements and can both activate and repress gene networks critical for epidermal barrier formation, wound repair, and neurulation. GRHL3 is also recognized as a pioneer factor, able to remodel chromatin to establish an epithelial transcriptional landscape and facilitate cellular differentiation. Loss-of-function mutations or dysregulation of GRHL3 are implicated in various developmental defects (e.g., cleft palate, neural tube defects, Van der Woude syndrome), as well as tumorigenesis, particularly through modulation of cell adhesion, migration, and the epithelial-mesenchymal transition. In cancer, GRHL3 most notably acts as a tumor suppressor in squamous cell carcinomas by regulating PTEN and other differentiation-related genes.

Other names

Grainyhead-like protein 3 homologSister of mammalian grainyheadTranscription factor CP2-like 4SOMTFCP2L4VWS2transcription factor hSOM1

Not applicable (no direct drug mechanisms currently established for specific GRHL3 targeting)