Issue 98, 2023

Utilising the intrinsic fluorescence of pomalidomide for imaging applications

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.

Graphical abstract: Utilising the intrinsic fluorescence of pomalidomide for imaging applications

Supplementary files

Article information

Article type
Communication
Submitted
31 Ago 2023
Accepted
22 Nov 2023
First published
29 Nov 2023

Chem. Commun., 2023,59, 14532-14535

Utilising the intrinsic fluorescence of pomalidomide for imaging applications

D. K. Brownsey, C. J. Gafuik, D. Kim, L. O’Sullivan, E. Gorobets, S. Krukowski, M. Turk, C. N. Jenne, D. J. Mahoney and D. J. Derksen, Chem. Commun., 2023, 59, 14532 DOI: 10.1039/D3CC04314B

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