Details

Autor(en) / Beteiligte

• Kounde, Cyrille S
• Shchepinova, Maria M
• Saunders, Charlie N
• Muelbaier, Marcel
• Rackham, Mark D
• Harling, John D
• Tate, Edward W

Titel

A caged E3 ligase ligand for PROTAC-mediated protein degradation with light

Ist Teil von

• Chemical communications (Cambridge, England), 2020-05, Vol.56 (41), p.5532-5535

Ort / Verlag

England: Royal Society of Chemistry

Erscheinungsjahr

2020

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• With the intent of achieving greater spatiotemporal control of PROTAC-induced protein degradation, a light-activated degrader was designed by photocaging an essential E3 ligase binding motif in a BRD4 targeting PROTAC. Proteolysis was triggered only after a short irradiation time, the kinetics of which could be monitored by live-cell video microscopy. Caging of a widely used Von Hippel Lindau E3 ligase ligand for targeted protein degradation with PROTACs allows light-activated proteolysis.