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Disrupting the Constitutive, Homodimeric Protein-Protein Interface in CK2β Using a Biophysical Fragment-Based Approach.

Accepted version
Peer-reviewed

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Abstract

Identifying small molecules that induce the disruption of constitutive protein-protein interfaces is a challenging objective. Here, a targeted biophysical screening cascade was employed to specifically identify small molecules that could disrupt the constitutive, homodimeric protein-protein interface within CK2β. This approach could potentially be applied to achieve subunit disassembly of other homo-oligomeric proteins as a means of modulating protein function.

Description

Journal Title

J Am Chem Soc

Conference Name

Journal ISSN

0002-7863
1520-5126

Volume Title

138

Publisher

American Chemical Society (ACS)

Rights and licensing

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Sponsorship
Wellcome Trust (090340/Z/09/Z)
Engineering and Physical Sciences Research Council (EP/K039520/1)
This research was supported by the Agency for Science, Technology and Research (A*STAR) Singapore (Ph.D. sponsorship, W.G.S.) and the Wellcome Trust Strategic Award (090340/Z/09/Z).