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...

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التفاصيل البيبلوغرافية
المؤلفون الرئيسيون: Cortopassi, W, Kumar, K, Paton, R
التنسيق: Journal article
منشور في: Royal Society of Chemistry 2016