A chemical probe for the ATAD2 bromodomain
Research output: Contribution to journal › Article › peer-review
ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.
| Original language | English |
|---|---|
| Pages (from-to) | 11382-11386 |
| Number of pages | 5 |
| Journal | Angewandte Chemie International Edition |
| Volume | 55 |
| Issue number | 38 |
| Early online date | 17 Aug 2016 |
| DOIs | |
| Publication status | Published - 12 Sep 2016 |
| Externally published | Yes |
Documents
- A Chemical Probe
Rights statement: This is the peer reviewed version of the following article: P. Bamborough, C.-w. Chung, E. H. Demont, R. C. Furze, A. J. Bannister, K. H. Che, H. Diallo, C. Douault, P. Grandi, T. Kouzarides, A.-M. Michon, D. J. Mitchell, R. K. Prinjha, C. Rau, S. Robson, R. J. Sheppard, R. Upton, R. J. Watson, Angew. Chem. Int. Ed. 2016, 55, 11382., which has been published in final form at http://onlinelibrary.wiley.com/doi/10.1002/anie.201603928/full. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving.
Accepted author manuscript (Post-print), 544 KB, PDF document
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