A Chemical Probe for the ATAD2 Bromodomain.
Angew Chem Int Ed Engl
; 55(38): 11382-6, 2016 09 12.
Article
en En
| MEDLINE
| ID: mdl-27530368
ABSTRACT
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.
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MEDLINE
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Año:
2016
Tipo del documento:
Article
País de afiliación:
Reino Unido