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1000 Titel
  • Anti-tumor effects of tirbanibulin in squamous cell carcinoma cells are mediated via disruption of tubulin-polymerization
1000 Autor/in
  1. DeTemple, Viola K. |
  2. Walter, Antje |
  3. Bredemeier-Rasche, Sabine |
  4. Gutzmer, Ralf |
  5. Schaper-Gerhardt, Katrin |
1000 Verlag
  • Springer Berlin Heidelberg
1000 Erscheinungsjahr 2024
1000 Publikationstyp
  1. Artikel |
1000 Online veröffentlicht
  • 2024-06-07
1000 Erschienen in
1000 Quellenangabe
  • 316(7):341
1000 Copyrightjahr
  • 2024
1000 Lizenz
1000 Verlagsversion
  • https://doi.org/10.1007/s00403-024-03032-x |
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11161541/ |
1000 Publikationsstatus
1000 Begutachtungsstatus
1000 Sprache der Publikation
1000 Abstract/Summary
  • <jats:title>Abstract</jats:title><jats:p>Topical tirbanibulin is a highly effective and well tolerated novel treatment option for actinic keratoses (AKs). This study aimed to characterize the mode of action of tirbanibulin in keratinocytes (NHEK) and cutaneous squamous cell carcinoma (cSCC) cell lines (A431, SCC-12) in vitro. Tirbanibulin significantly reduced proliferation in a dose-dependent manner in all investigated cell lines, inhibited migration, and induced G2/M-cell cycle arrest only in the cSCC cell lines analyzed, and induced apoptosis solely in A431, which showed the highest sensitivity to tirbanibulin. In general, we detected low basal expression of phosphorylated SRC in all cell lines analyzed, therefore, interference with SRC signaling does not appear to be the driving force regarding the observed effects of tirbanibulin. The most prominent tirbanibulin-mediated effect was on β-tubulin-polymerization, which was especially impaired in A431. Additionally, tirbanibulin induced an increase of the proinflammatory cytokines IL-1α, bFGF and VEGF in A431. In conclusion, tirbanibulin mediated anti-tumor effects predominantly in A431, while healthy keratinocytes and more dedifferentiated SCC-12 were less influenced. These effects of tirbanibulin are most likely mediated via dysregulation of β-tubulin-polymerization and may be supported by proinflammatory aspects.</jats:p>
1000 Sacherschließung
lokal Pyridines [MeSH]
lokal Cell Line, Tumor [MeSH]
lokal Beta-tubulin-polymerization
lokal Antineoplastic Agents/pharmacology [MeSH]
lokal Keratinocytes/drug effects [MeSH]
lokal Skin Neoplasms/drug therapy [MeSH]
lokal Cell Movement/drug effects [MeSH]
lokal Morpholines [MeSH]
lokal Keratinocytes/metabolism [MeSH]
lokal Tirbanibulin,
lokal Keratosis, Actinic/drug therapy [MeSH]
lokal Signal Transduction/drug effects [MeSH]
lokal Skin Neoplasms/metabolism [MeSH]
lokal Carcinoma, Squamous Cell/pathology [MeSH]
lokal Keratosis, Actinic/pathology [MeSH]
lokal Polymerization/drug effects [MeSH]
lokal Actinic keratosis (AK)
lokal Humans [MeSH]
lokal Apoptosis/drug effects [MeSH]
lokal Tubulin/metabolism [MeSH]
lokal Skin Neoplasms/pathology [MeSH]
lokal Carcinoma, Squamous Cell/drug therapy [MeSH]
lokal Cutaneous squamous cell carcinoma (cSCC)
lokal Acetamides [MeSH]
lokal Keratosis, Actinic/metabolism [MeSH]
lokal Original Paper
lokal Cell Proliferation/drug effects [MeSH]
lokal Carcinoma, Squamous Cell/metabolism [MeSH]
1000 Fächerklassifikation (DDC)
1000 Liste der Beteiligten
  1. https://orcid.org/0000-0001-6246-8862|https://orcid.org/0009-0007-5970-7755|https://orcid.org/0009-0005-0950-8323|https://orcid.org/0000-0001-7921-2820|https://orcid.org/0000-0002-5318-0039
1000 Hinweis
  • DeepGreen-ID: 6981ae172f284a458c2be8e8e9f1efda ; metadata provieded by: DeepGreen (https://www.oa-deepgreen.de/api/v1/), LIVIVO search scope life sciences (http://z3950.zbmed.de:6210/livivo), Crossref Unified Resource API (https://api.crossref.org/swagger-ui/index.html), to.science.api (https://frl.publisso.de/), ZDB JSON-API (beta) (https://zeitschriftendatenbank.de/api/), lobid - Dateninfrastruktur für Bibliotheken (https://lobid.org/resources/search)
1000 Label
1000 Förderer
  1. Almirall |
  2. Ruhr-Universität Bochum |
1000 Fördernummer
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1000 Dateien
1000 Förderung
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    1000 Förderer Almirall |
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    1000 Fördernummer -
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    1000 Förderer Ruhr-Universität Bochum |
    1000 Förderprogramm -
    1000 Fördernummer -
1000 Objektart article
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1000 @id frl:6500757.rdf
1000 Erstellt am 2025-02-05T10:56:52.782+0100
1000 Erstellt von 322
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1000 Zuletzt bearbeitet 2025-07-30T08:24:36.448+0200
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