G4-Ligand-Directed PROTACs Unveil DR1 as a Novel Ligand-Co-Binding G4-Protein and Reshape G4-Dependent Transcription - PubMed
3 days ago
- #targeted protein degradation
- #G4-binding proteins
- #transcription regulation
- G4-Ligand-Directed PROTACs (G4L-TACs) introduced as a platform to degrade ligand-co-binding G4-binding proteins (G4BPs).
- DR1 identified as a novel G4BP recruited to ligand-stabilized promoter G4s using PDS-derived G4L-TACs.
- G4L-TAC-mediated DR1 degradation relieves transcriptional repression at G4-rich oncogenic promoters.
- Study provides insights into how G4 ligands influence gene expression beyond nucleic acid stabilization.
- G4L-TACs serve as a tool for discovering ligand-co-binding G4BPs and exploring therapeutic potential.