NJH-2-057 is a novel CFTR DUBTAC via linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor with C5 alkyl linkers.
NJH-2-057 robustly stabilizes ΔF508-CFTR protein levels, leading to improved chloride channel conductance in human cystic fibrosis bronchial epithelial cells.
Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner.
