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

[Image: see text] 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 protei...

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Detalles Bibliográficos
Autores principales: Seetoh, Wei-Guang, Abell, Chris
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5257173/
https://www.ncbi.nlm.nih.gov/pubmed/27726344
http://dx.doi.org/10.1021/jacs.6b07440
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author Seetoh, Wei-Guang
Abell, Chris
author_facet Seetoh, Wei-Guang
Abell, Chris
author_sort Seetoh, Wei-Guang
collection PubMed
description [Image: see text] 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.
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spelling pubmed-52571732017-01-24 Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach Seetoh, Wei-Guang Abell, Chris J Am Chem Soc [Image: see text] 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. American Chemical Society 2016-10-11 2016-11-02 /pmc/articles/PMC5257173/ /pubmed/27726344 http://dx.doi.org/10.1021/jacs.6b07440 Text en Copyright © 2016 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Seetoh, Wei-Guang
Abell, Chris
Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title_full Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title_fullStr Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title_full_unstemmed Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title_short Disrupting the Constitutive, Homodimeric Protein–Protein Interface in CK2β Using a Biophysical Fragment-Based Approach
title_sort disrupting the constitutive, homodimeric protein–protein interface in ck2β using a biophysical fragment-based approach
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5257173/
https://www.ncbi.nlm.nih.gov/pubmed/27726344
http://dx.doi.org/10.1021/jacs.6b07440
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