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

Cyrille S KoundeMaria M ShchepinovaCharlie N Saunders Marcel MuelbaierMark D RackhamJohn D Harling Edward William Tate

Published in: Chemical communications (Cambridge, England) (2020)

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.

Keyphrases

binding protein
protein protein
amino acid
high glucose
diabetic rats
optical coherence tomography
transcription factor
small molecule
oxidative stress
dna binding
mass spectrometry
single cell
electron microscopy