Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.

Transcriptional activation domains (ADs) are generally thought to be intrinsically unstructured, but capable of adopting limited secondary structure upon interaction with a coactivator surface. The indeterminate nature of this interface made it hitherto difficult to study structure/function relation...

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Main Authors: Natalie S Scholes, Robert O J Weinzierl
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2016-05-01
Series:PLoS Computational Biology
Online Access:https://journals.plos.org/ploscompbiol/article/file?id=10.1371/journal.pcbi.1004935&type=printable
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author Natalie S Scholes
Robert O J Weinzierl
author_facet Natalie S Scholes
Robert O J Weinzierl
author_sort Natalie S Scholes
collection DOAJ
description Transcriptional activation domains (ADs) are generally thought to be intrinsically unstructured, but capable of adopting limited secondary structure upon interaction with a coactivator surface. The indeterminate nature of this interface made it hitherto difficult to study structure/function relationships of such contacts. Here we used atomistic accelerated molecular dynamics (aMD) simulations to study the conformational changes of the GCN4 AD and variants thereof, either free in solution, or bound to the GAL11 coactivator surface. We show that the AD-coactivator interactions are highly dynamic while obeying distinct rules. The data provide insights into the constant and variable aspects of orientation of ADs relative to the coactivator, changes in secondary structure and energetic contributions stabilizing the various conformers at different time points. We also demonstrate that a prediction of α-helical propensity correlates directly with the experimentally measured transactivation potential of a large set of mutagenized ADs. The link between α-helical propensity and the stimulatory activity of ADs has fundamental practical and theoretical implications concerning the recruitment of ADs to coactivators.
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spelling doaj-art-8c416b49fbd64c4b83f874c19d3272a92025-08-20T03:24:36ZengPublic Library of Science (PLoS)PLoS Computational Biology1553-734X1553-73582016-05-01125e100493510.1371/journal.pcbi.1004935Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.Natalie S ScholesRobert O J WeinzierlTranscriptional activation domains (ADs) are generally thought to be intrinsically unstructured, but capable of adopting limited secondary structure upon interaction with a coactivator surface. The indeterminate nature of this interface made it hitherto difficult to study structure/function relationships of such contacts. Here we used atomistic accelerated molecular dynamics (aMD) simulations to study the conformational changes of the GCN4 AD and variants thereof, either free in solution, or bound to the GAL11 coactivator surface. We show that the AD-coactivator interactions are highly dynamic while obeying distinct rules. The data provide insights into the constant and variable aspects of orientation of ADs relative to the coactivator, changes in secondary structure and energetic contributions stabilizing the various conformers at different time points. We also demonstrate that a prediction of α-helical propensity correlates directly with the experimentally measured transactivation potential of a large set of mutagenized ADs. The link between α-helical propensity and the stimulatory activity of ADs has fundamental practical and theoretical implications concerning the recruitment of ADs to coactivators.https://journals.plos.org/ploscompbiol/article/file?id=10.1371/journal.pcbi.1004935&type=printable
spellingShingle Natalie S Scholes
Robert O J Weinzierl
Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
PLoS Computational Biology
title Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
title_full Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
title_fullStr Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
title_full_unstemmed Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
title_short Molecular Dynamics of "Fuzzy" Transcriptional Activator-Coactivator Interactions.
title_sort molecular dynamics of fuzzy transcriptional activator coactivator interactions
url https://journals.plos.org/ploscompbiol/article/file?id=10.1371/journal.pcbi.1004935&type=printable
work_keys_str_mv AT nataliesscholes moleculardynamicsoffuzzytranscriptionalactivatorcoactivatorinteractions
AT robertojweinzierl moleculardynamicsoffuzzytranscriptionalactivatorcoactivatorinteractions