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JoVE Journal Chemistry
Inattivazione chimica dell'E3 Ubiquitin Ligase Cereblon da parte di Homo-PROTAC con sede a Pomeredomide
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Inattivazione chimica dell'E3 Ubiquitin Ligase Cereblon da parte di Homo-PROTAC con sede a Pomeredomide

Article DOI: 10.3791/59472-v • 10:44 min • May 15th, 2019
May 15th, 2019 •
*1, *2, 1, 2, 2, 1
1Department of Internal Medicine III, University Hospital Ulm, 2Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn
* These authors contributed equally

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Questo lavoro descrive la sintesi e la caratterizzazione di un omo-PROTAC bimalidomide a base di pomalimmide come un nuovo approccio per indurre l'ubiquitinazione e la degradazione della cereblon della ligase dell'ubiquitina E3 (CRBN), l'obiettivo degli analoghi di talidomide.

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Chimica Numero 147 CRBN PROTAC IMiD pomalidomide ubiquitina ligase mieloma multiplo proteasome
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