Development of the first geldanamycin-based HSP90 degraders
Development of the first geldanamycin-based HSP90 degraders
Dokument öffnen (1.6MB)Datum der Veröffentlichung
28.06.2023Verlag / herausgebende Einrichtung
Frontiers MediaVerlagsort
LausanneMetadaten
Zur Langanzeige
Zitierbarer Link (Handle URI) 
https://hdl.handle.net/20.500.11811/12817
Inhalt
Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting chimeras (PROTACs) to degrade the protein instead of inhibiting it may overcome these problems. In this work, we describe the design, synthesis, and evaluation of cereblon-recruiting geldanamycin-based HSP90 degraders based on the PROTAC technology. Our best degrader, 3a, effectively decreased HSP90α and HSP90β levels in cells utilizing the ubiquitin–proteasome pathway.
Schlagwörter
cancer, cereblon, heat shock protein, Hsp90, PROTAC
Klassifikation (DDC)
540 ChemieErschienen in
Frontiers in Chemistry, 2023, vol. 11, 1219883, S. 1-10Erstpublikation
https://doi.org/10.3389/fchem.2023.1219883Wurnig, Silas; Vogt, Melina; Hogenkamp, Julian; Dienstbier, Niklas; Borkhardt, Arndt; Bhatia, Sanil; Hansen, Finn: Development of the first geldanamycin-based HSP90 degraders. In: Frontiers in Chemistry. 2023, vol. 11, 1219883, 1-10.
Online-Ausgabe in bonndoc: https://hdl.handle.net/20.500.11811/12817
Online-Ausgabe in bonndoc: https://hdl.handle.net/20.500.11811/12817
@article{handle:20.500.11811/12817,
author = {{Silas Wurnig} and {Melina Vogt} and {Julian Hogenkamp} and {Niklas Dienstbier} and {Arndt Borkhardt} and {Sanil Bhatia} and {Finn Hansen}},
title = {Development of the first geldanamycin-based HSP90 degraders},
publisher = {Frontiers Media},
year = 2023,
month = jun,
journal = {Frontiers in Chemistry},
volume = 2023, vol. 11,
number = 1219883,
pages = 1--10,
note = {Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting chimeras (PROTACs) to degrade the protein instead of inhibiting it may overcome these problems. In this work, we describe the design, synthesis, and evaluation of cereblon-recruiting geldanamycin-based HSP90 degraders based on the PROTAC technology. Our best degrader, 3a, effectively decreased HSP90α and HSP90β levels in cells utilizing the ubiquitin–proteasome pathway.},
url = {https://hdl.handle.net/20.500.11811/12817}
}
author = {{Silas Wurnig} and {Melina Vogt} and {Julian Hogenkamp} and {Niklas Dienstbier} and {Arndt Borkhardt} and {Sanil Bhatia} and {Finn Hansen}},
title = {Development of the first geldanamycin-based HSP90 degraders},
publisher = {Frontiers Media},
year = 2023,
month = jun,
journal = {Frontiers in Chemistry},
volume = 2023, vol. 11,
number = 1219883,
pages = 1--10,
note = {Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting chimeras (PROTACs) to degrade the protein instead of inhibiting it may overcome these problems. In this work, we describe the design, synthesis, and evaluation of cereblon-recruiting geldanamycin-based HSP90 degraders based on the PROTAC technology. Our best degrader, 3a, effectively decreased HSP90α and HSP90β levels in cells utilizing the ubiquitin–proteasome pathway.},
url = {https://hdl.handle.net/20.500.11811/12817}
}
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