Projects per year
Abstract
The development and optimisation of a photoaffinity labelling (PAL) displacement assay is presented, where a highly efficient PAL probe was used to report on the relative binding affinities of compounds to specific binding sites in multiple recombinant protein domains in tandem. The N- and C-terminal bromodomains of BRD4 were used as example target proteins. A test set of 264 compounds annotated with activity against the bromodomain and extra-terminal domain (BET) family in ChEMBL were used to benchmark the assay. The pIC50 values obtained from the assay correlated well with orthogonal TR‑FRET data, highlighting the potential of this highly accessible PAL biochemical screening platform.
Original language | English |
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Pages (from-to) | 1183-1197 |
Number of pages | 15 |
Journal | Biochemical Journal |
Volume | 480 |
Issue number | 15 |
Early online date | 4 Jul 2023 |
DOIs | |
Publication status | Published - 31 Aug 2023 |
Keywords
- photoaffinity
- assay
- bromodomains
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Dive into the research topics of 'Photoaffinity labelling displacement assay using multiple recombinant protein domains'. Together they form a unique fingerprint.Projects
- 1 Finished
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Accelerated Discovery and Development of New Medicines: Prosperity Partnership for a Healthier Nation
Kerr, W. (Principal Investigator), Brown, C. (Co-investigator), Florence, A. (Co-investigator), Jamieson, C. (Co-investigator), Johnston, B. (Co-investigator), Murphy, J. (Co-investigator), Palmer, D. (Co-investigator) & Tomkinson, N. (Co-investigator)
EPSRC (Engineering and Physical Sciences Research Council)
1/01/19 → 30/09/24
Project: Research