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Comment
. 2012 Sep 13;55(17):7342-5.
doi: 10.1021/jm3011977. Epub 2012 Aug 28.

Scaling the druggability landscape of human bromodomains, a new class of drug targets

Guangtao Zhang  1 , Roberto Sanchez, Ming-Ming Zhou
Affiliations
Comment

Scaling the druggability landscape of human bromodomains, a new class of drug targets

Guangtao Zhang et al. J Med Chem. .
No abstract available

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Figures

Figure 1
Figure 1. Structural features of the acetyl-lysine binding pocket of the bromodomain
(A) The three-dimensional structure of the first bromodomain of human BRD4 (BRD4-BD1) (pdb code 3mxf), illustrating key amino acid residues, and five bound water molecules located at the acetyl-lysine binding pocket. The side chains of these residues are color-coded by atom type. (B) Surface representation of the BRD4-BD1 that is colored according to amino acid sequence conservation over the entire human bromodomain family (green is more conserved, whereas white is not conserved). (C) Acetyl-lysine (left) and a small molecule bromodomain inhibitor, JQ1 (right) shown when bound in the acetyl-lysine binding pocket (pdb codes 3uvx and 3mxf, respectively). The ligands, as well as bound water molecules are depicted in colored spheres according to atom type (red, blue, green, yellow and white for oxygen, nitrogen, carbon, sulfur, and hydrogen, respectively). The ligand binding site in the bromodomain protein is defined by mesh.
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