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 אוג 2023
Accepted
22 נוב 2023
First published
29 נוב 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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements