Author
Keywords
Abstract

Bromodomains are protein modules that selectively recognize histones by binding to acetylated lysines. Here, we have carried out multiple molecular dynamics simulations of 20 human bromodomains to investigate the flexibility of their binding site. Some bromodomains show alternative side chain orientations of three evolutionarily conserved residues: the Asn involved in acetyl-lysine binding and two conserved aromatic residues. Furthermore, for the BAZ2B and CREBBP bromodomains we observe occlusion of the binding site which is coupled to the displacement of the two aromatic residues. In contrast to available structures, the simulations reveal large variability of the binding site accessibility. The simulations suggest that the flexibility of the bromodomain binding site and presence of self-occluded metastable states influence the recognition of acetyl-lysine on histone tails.

Year of Publication
2013
Journal
FEBS Letters
Volume
587
Issue
14
Number of Pages
2158-2163
Date Published
2013 Jul 11
Type of Article
Research Article
ISSN Number
1873-3468
DOI
10.1016/j.febslet.2013.05.032
Alternate Journal
FEBS Lett.
PMID
23711371
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