Publikation:

Conformational selection vs. induced fit : insights into the binding mechanisms of p38α MAP Kinase inhibitors

Lade...
Vorschaubild

Dateien

Roser_2-tskeesl8c0w13.pdf
Roser_2-tskeesl8c0w13.pdfGröße: 2.18 MBDownloads: 183

Datum

2020

Autor:innen

Herausgeber:innen

Kontakt

ISSN der Zeitschrift

Electronic ISSN

ISBN

Bibliografische Daten

Verlag

Schriftenreihe

Auflagebezeichnung

DOI (zitierfähiger Link)
ArXiv-ID

Internationale Patentnummer

Angaben zur Forschungsförderung

Projekt

Open Access-Veröffentlichung
Open Access Hybrid
Core Facility der Universität Konstanz

Gesperrt bis

Titel in einer weiteren Sprache

Publikationstyp
Zeitschriftenartikel
Publikationsstatus
Published

Erschienen in

Chemical Communications. Royal Society of Chemistry (RSC). 2020, 56(62), pp. 8818-8821. ISSN 1359-7345. eISSN 1364-548X. Available under: doi: 10.1039/d0cc02539a

Zusammenfassung

The conformational dynamics of a kinase's activation loop have been challenging to assess due to the activation loop's intrinsic flexibility. To directly probe the conformational equilibrium of the activation loop of mitogen-activated protein kinase p38α, we present an approach based on site-directed spin labeling, electron paramagnetic resonance (EPR) distance restraints, and multilateration. We demonstrate that the activation loop of apo p38α resides in a highly flexible equilibrium state and we reveal that binding of small molecules significantly alters this equilibrium and the populated sub-states.

Zusammenfassung in einer weiteren Sprache

Fachgebiet (DDC)
540 Chemie

Schlagwörter

Konferenz

Rezension
undefined / . - undefined, undefined

Forschungsvorhaben

Organisationseinheiten

Zeitschriftenheft

Zugehörige Datensätze in KOPS

Zitieren

ISO 690ROSER, Patrick, Jörn WEISNER, Juliane STEHLE, Daniel RAUH, Malte DRESCHER, 2020. Conformational selection vs. induced fit : insights into the binding mechanisms of p38α MAP Kinase inhibitors. In: Chemical Communications. Royal Society of Chemistry (RSC). 2020, 56(62), pp. 8818-8821. ISSN 1359-7345. eISSN 1364-548X. Available under: doi: 10.1039/d0cc02539a
BibTex
@article{Roser2020-08-04Confo-50925,
  year={2020},
  doi={10.1039/d0cc02539a},
  title={Conformational selection vs. induced fit : insights into the binding mechanisms of p38α MAP Kinase inhibitors},
  number={62},
  volume={56},
  issn={1359-7345},
  journal={Chemical Communications},
  pages={8818--8821},
  author={Roser, Patrick and Weisner, Jörn and Stehle, Juliane and Rauh, Daniel and Drescher, Malte}
}
RDF
<rdf:RDF
    xmlns:dcterms="http://purl.org/dc/terms/"
    xmlns:dc="http://purl.org/dc/elements/1.1/"
    xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#"
    xmlns:bibo="http://purl.org/ontology/bibo/"
    xmlns:dspace="http://digital-repositories.org/ontologies/dspace/0.1.0#"
    xmlns:foaf="http://xmlns.com/foaf/0.1/"
    xmlns:void="http://rdfs.org/ns/void#"
    xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > 
  <rdf:Description rdf:about="https://kops.uni-konstanz.de/server/rdf/resource/123456789/50925">
    <dspace:hasBitstream rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/50925/1/Roser_2-tskeesl8c0w13.pdf"/>
    <dcterms:issued>2020-08-04</dcterms:issued>
    <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/50925"/>
    <dspace:isPartOfCollection rdf:resource="https://kops.uni-konstanz.de/server/rdf/resource/123456789/29"/>
    <dcterms:isPartOf rdf:resource="https://kops.uni-konstanz.de/server/rdf/resource/123456789/29"/>
    <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2020-09-21T12:25:56Z</dc:date>
    <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2020-09-21T12:25:56Z</dcterms:available>
    <dc:language>eng</dc:language>
    <dc:contributor>Roser, Patrick</dc:contributor>
    <dc:creator>Roser, Patrick</dc:creator>
    <dcterms:rights rdf:resource="http://creativecommons.org/licenses/by/3.0/"/>
    <dcterms:abstract xml:lang="eng">The conformational dynamics of a kinase's activation loop have been challenging to assess due to the activation loop's intrinsic flexibility. To directly probe the conformational equilibrium of the activation loop of mitogen-activated protein kinase p38α, we present an approach based on site-directed spin labeling, electron paramagnetic resonance (EPR) distance restraints, and multilateration. We demonstrate that the activation loop of apo p38α resides in a highly flexible equilibrium state and we reveal that binding of small molecules significantly alters this equilibrium and the populated sub-states.</dcterms:abstract>
    <dc:creator>Weisner, Jörn</dc:creator>
    <dc:creator>Drescher, Malte</dc:creator>
    <void:sparqlEndpoint rdf:resource="http://localhost/fuseki/dspace/sparql"/>
    <dcterms:title>Conformational selection vs. induced fit : insights into the binding mechanisms of p38α MAP Kinase inhibitors</dcterms:title>
    <dc:rights>Attribution 3.0 Unported</dc:rights>
    <dc:creator>Stehle, Juliane</dc:creator>
    <dcterms:hasPart rdf:resource="https://kops.uni-konstanz.de/bitstream/123456789/50925/1/Roser_2-tskeesl8c0w13.pdf"/>
    <dc:contributor>Drescher, Malte</dc:contributor>
    <dc:contributor>Rauh, Daniel</dc:contributor>
    <dc:contributor>Stehle, Juliane</dc:contributor>
    <dc:creator>Rauh, Daniel</dc:creator>
    <foaf:homepage rdf:resource="http://localhost:8080/"/>
    <dc:contributor>Weisner, Jörn</dc:contributor>
  </rdf:Description>
</rdf:RDF>

Interner Vermerk

xmlui.Submission.submit.DescribeStep.inputForms.label.kops_note_fromSubmitter

Kontakt
URL der Originalveröffentl.

Prüfdatum der URL

Prüfungsdatum der Dissertation

Finanzierungsart

Kommentar zur Publikation

Allianzlizenz
Corresponding Authors der Uni Konstanz vorhanden
Internationale Co-Autor:innen
Universitätsbibliographie
Ja
Begutachtet
Ja
Diese Publikation teilen