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1000 Titel
  • Identification and characterization of deschloro-chlorothricin obtained from a large natural product library targeting aurora A kinase in multiple myeloma
1000 Autor/in
  1. Özenver, Nadire |
  2. Abdelfatah, Sara |
  3. Klinger, Anette |
  4. Fleischer, Edmond |
  5. Efferth, Thomas |
1000 Erscheinungsjahr 2020
1000 Publikationstyp
  1. Artikel |
1000 Online veröffentlicht
  • 2020-09-25
1000 Erschienen in
1000 Quellenangabe
  • 39(2):348-361
1000 Copyrightjahr
  • 2020
1000 Lizenz
1000 Verlagsversion
  • https://doi.org/10.1007/s10637-020-01012-2 |
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8551148/ |
1000 Publikationsstatus
1000 Sprache der Publikation
1000 Abstract/Summary
  • Multiple myeloma (MM) is a devastating disease with low survival rates worldwide. The mean lifetime of patients may be extendable with new drug alternatives. Aurora A kinase (AURKA) is crucial in oncogenesis, because its overexpression or amplification may incline the development of various types of cancer, including MM. Therefore, inhibitors of AURKA are innovative and promising targets. Natural compounds always represented a valuable resource for anticancer drug development. In the present study, based on virtual drug screening of more than 48,000 natural compounds, the antibiotic deschloro-chlorotricin (DCCT) has been identified to bind to AURKA with even higher binding affinity (free bindung energy: -12.25 kcal/mol) than the known AURKA inhibitor, alisertib (free binding energy: -11.25 kcal/mol). The in silico studies have been verified in vitro by using microscale thermophoresis. DCCT inhibited MM cell lines (KMS-11, L-363, RPMI-8226, MOLP-8, OPM-2, NCI-H929) with IC
1000 Sacherschließung
lokal Azepines/antagonists
lokal Dose-Response Relationship, Drug [MeSH]
lokal Pyrimidines/pharmacology [MeSH]
lokal Multiple myeloma
lokal Cell Line, Tumor [MeSH]
lokal Aurora Kinase A/antagonists
lokal Cancer
lokal Humans [MeSH]
lokal Aminoglycosides/pharmacology [MeSH]
lokal Targeted chemotherapy
lokal Pyrimidines/antagonists
lokal Azepines/pharmacology [MeSH]
lokal Preclinical Studies
lokal Protein Binding/physiology [MeSH]
lokal Multiple Myeloma/drug therapy [MeSH]
lokal Natural product, precision medicine
lokal Cell Cycle [MeSH]
1000 Liste der Beteiligten
  1. https://orcid.org/0000-0001-9561-8994|https://orcid.org/0000-0002-9186-2516|https://frl.publisso.de/adhoc/uri/S2xpbmdlciwgQW5ldHRl|https://frl.publisso.de/adhoc/uri/RmxlaXNjaGVyLCBFZG1vbmQ=|https://orcid.org/0000-0002-2637-1681
1000 Hinweis
  • DeepGreen-ID: 9ed48ef77ca342e1b79c78068aebe839 ; 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)
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1000 @id frl:6468394.rdf
1000 Erstellt am 2023-11-17T16:06:49.229+0100
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1000 Zuletzt bearbeitet Fri Dec 01 07:49:58 CET 2023
1000 Objekt bearb. Fri Dec 01 07:49:58 CET 2023
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