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Titel:

PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase

Dokumenttyp:
Zeitschriftenaufsatz
Autor(en):
Adhikari, Bikash; Bozilovic, Jelena; Diebold, Mathias; Schwarz, Jessica Denise; Hofstetter, Julia; Schröder, Martin; Wanior, Marek; Narain, Ashwin; Vogt, Markus; Dudvarski Stankovic, Nevenka; Baluapuri, Apoorva; Schönemann, Lars; Eing, Lorenz; Bhandare, Pranjali; Kuster, Bernhard; Schlosser, Andreas; Heinzlmeir, Stephanie; Sotriffer, Christoph; Knapp, Stefan; Wolf, Elmar
Abstract:
The mitotic kinase AURORA-A is essential for cell cycle progression and is considered a priority cancer target. Although the catalytic activity of AURORA-A is essential for its mitotic function, recent reports indicate an additional non-catalytic function, which is difficult to target by conventional small molecules. We therefore developed a series of chemical degraders (PROTACs) by connecting a clinical kinase inhibitor of AURORA-A to E3 ligase-binding molecules (for example, thalidomide). One...     »
Stichworte:
BayBioMS; cancer; cell division; Kinases; Medicinal chemistry; small molecules
Zeitschriftentitel:
Nature Chemical Biology
Jahr:
2020
Volltext / DOI:
doi:10.1038/s41589-020-00652-y
Verlag / Institution:
Springer Science and Business Media LLC
E-ISSN:
1552-44501552-4469
Publikationsdatum:
28.09.2020
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