1 Ocak 1999 Dergi makalesi Açık Erişim

Rungeler, P; Castro, V; Mora, G; Goren, N; Vichnewski, W; Pahl, HL; Merfort, I; Schmidt, TJ

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/101601</identifier>
  <creators>
    <creator>
      <creatorName>Rungeler, P</creatorName>
      <givenName>P</givenName>
      <familyName>Rungeler</familyName>
    </creator>
    <creator>
      <creatorName>Castro, V</creatorName>
      <givenName>V</givenName>
      <familyName>Castro</familyName>
    </creator>
    <creator>
      <creatorName>Mora, G</creatorName>
      <givenName>G</givenName>
      <familyName>Mora</familyName>
    </creator>
    <creator>
      <creatorName>Goren, N</creatorName>
      <givenName>N</givenName>
      <familyName>Goren</familyName>
    </creator>
    <creator>
      <creatorName>Vichnewski, W</creatorName>
      <givenName>W</givenName>
      <familyName>Vichnewski</familyName>
    </creator>
    <creator>
      <creatorName>Pahl, HL</creatorName>
      <givenName>HL</givenName>
      <familyName>Pahl</familyName>
    </creator>
    <creator>
      <creatorName>Merfort, I</creatorName>
      <givenName>I</givenName>
      <familyName>Merfort</familyName>
    </creator>
    <creator>
      <creatorName>Schmidt, TJ</creatorName>
      <givenName>TJ</givenName>
      <familyName>Schmidt</familyName>
    </creator>
  </creators>
  <titles>
    <title>Inhibition Of Transcription Factor Nf-Kappa B By Sesquiterpene Lactones: A Proposed Molecular Mechanism Of Action</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>1999</publicationYear>
  <dates>
    <date dateType="Issued">1999-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/101601</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsVersionOf">10.81043/aperta.101600</relatedIdentifier>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.81043/aperta.101601</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by">Creative Commons Attribution</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">Many sesquiterpene lactones (SLs) possess considerable anti-inflammatory activity. They inhibit the transcription factor NF-kappa B by selectively alkylating its p65 subunit probably by reacting with cysteine residues. Here we assayed 28 sesquiterpene lactones for their ability to inhibit NF-kappa B. The majority of the potent NF-kappa B inhibitors possess two reactive centers in form of an amethylene-gamma-lactone group and an alpha,beta- or alpha,beta,gamma,delta-unsaturated carbonyl group. Based on computer molecular modelling we propose a molecular mechanism of action, which is able to explain the p65 selectivity of the SLs and the observed correlation of high activity with alkylant bifunctionality. A single bifunctional SL molecule can alkylate the cysteine residue (Cys 38) in the DNA binding loop 1 (L1) and a further cysteine (Cys 120) in the nearby E' region. This cross link alters the position of tyrosine 36 and additional amino acids in such a way that their specific interactions with the DNA become impossible. We also created a model for monofunctional SLs. (C) 1999 Elsevier Science Ltd. All rights reserved.</description>
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