5A5S: Nn-terminal Bromodomain Of Human Brd4 With 5-5- Methoxypyridin-3-yl-3-methyl-8-piperidin-4-ylamino-1,2- Dihydro-1,7-naphthyridin-2-one

Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors limits clear understanding of the therapeutic potential of the bromodomain. Here, we describe the discovery of a hit from a fragment-based targeted array. Optimization of this produced the first known micromolar inhibitors of the ATAD2 bromodomain.
PDB ID: 5A5SDownload
MMDB ID: 131168
PDB Deposition Date: 2015/6/20
Updated in MMDB: 2015/08
Experimental Method:
x-ray diffraction
Resolution: 1.36  Å
Source Organism:
Similar Structures:
Biological Unit for 5A5S: monomeric; determined by author and by software (PISA)
Molecular Components in 5A5S
Label Count Molecule
Protein (1 molecule)
Bromodomain-containing Protein 4(Gene symbol: BRD4)
Molecule annotation
Chemicals (2 molecules)
* Click molecule labels to explore molecular sequence information.

Citing MMDB