5FE9: Crystal Structure Of Human Pcaf Bromodomain In Complex With Compound Sl1122 (compound 13)

Citation:
Abstract
The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.
PDB ID: 5FE9Download
MMDB ID: 135557
PDB Deposition Date: 2015/12/16
Updated in MMDB: 2016/04
Experimental Method:
x-ray diffraction
Resolution: 2.35  Å
Source Organism:
Similar Structures:
Biological Unit for 5FE9: monomeric; determined by author
Molecular Components in 5FE9
Label Count Molecule
Protein (1 molecule)
1
Histone Acetyltransferase Kat2b(Gene symbol: KAT2B)
Molecule annotation
Chemicals (2 molecules)
1
1
2
1
* Click molecule labels to explore molecular sequence information.

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