Cation–π interactions in CREBBP bromodomain inhibition - an electrostatic model for small molecule binding affinity and selectivity
CREBBP bromodomains, epigenetic “reader” proteins that recognize acetylated histone lysine residues, are a current target for cancer therapy. We show that experimental CREBBP binding affinities of small-molecules with aromatic or heteroaromatic functional groups are strongly influenced by a cation–π...
| Main Authors: | , , |
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| Format: | Journal article |
| Published: |
Royal Society of Chemistry
2016
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