TLE family member 1, transcriptional corepressor (TLE1)

TLE family member 1, transcriptional corepressor (TLE1), is a nuclear protein that acts as a transcriptional corepressor. It interacts with a variety of DNA-binding transcription factors and is crucial in regulating gene expression by repressing target genes, often through the recruitment of chromatin-modifying enzymes including histone deacetylases[2][5]. TLE1 plays roles in developmental processes, stem cell maintenance, cell fate decisions, and suppression of apoptosis and inflammation[3][5]. In cancer, TLE1 promotes epithelial-mesenchymal transition (EMT), resistance to apoptosis, and therapy resistance—particularly in lung adenocarcinoma, where its overexpression predicts poor prognosis and resistance to EGFR-TKIs such as gefitinib[1]. Loss of TLE1 induces proinflammatory cytokine production and can accelerate tumor progression, highlighting its dual roles in inflammation control and tumorigenesis[3][5]. No direct small-molecule inhibitors have been clinically approved, but modulation via chromatin regulators (e.g., HDAC inhibitors) and biomarker-driven selection strategies are areas of active research[1][5].

Other names

Transducin-like enhancer protein 1ESG1GRG1TLE-1E(Sp1) homologEnhancer of split groucho-like protein 1enhancer of split groucho 1ESGtransducin-like enhancer of split 1enhancer of split groucho-like protein 1transducin like enhancer of split 1

Inhibition of TLE1 nuclear function (proposed), Epigenetic modulation through corepressor complexes (e.g., with HDAC), Modulation of EMT and apoptosis-related transcriptional programs