Utilising the intrinsic fluorescence of pomalidomide for imaging applications

Chem Commun (Camb). 2023 Dec 7;59(98):14532-14535. doi: 10.1039/d3cc04314b.

Abstract

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.

MeSH terms

  • Microscopy, Fluorescence
  • Thalidomide* / pharmacology

Substances

  • pomalidomide
  • Thalidomide