TY - JOUR
AU - Derksen, Darren J.
AB - Optimisation of protein degraders requires balancing multiple factors including potency, cell permeability and solubility. Here we show that the fluorescence of pomalidomide can be used in high-throughput screening assays to rapidly assess cellular penetration of degrader candidates. In addition, this technique can be paired with endocytosis inhibitors to gain insight into potential mechanisms of candidates entering a target cell. A model library of pomalidomide conjugates was synthesised and evaluated using high-throughput fluorescence microscopy. This technique based on intrinsic fluorescence can be used to guide rational design of pomalidomide conjugates without the need for additional labels or tags.
TI - Utilising the intrinsic fluorescence of pomalidomide for imaging applications
JF - Chemical Communications
DO - 10.1039/d3cc04314b
DA - 2023-12-07
UR - https://www.deepdyve.com/lp/royal-society-of-chemistry/utilising-the-intrinsic-fluorescence-of-pomalidomide-for-imaging-ALbwl4FTiz
SP - 14532
EP - 14535
VL - 59
IS - 98
DP - DeepDyve
ER -