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Chemische inactivatie van de E3 Ubiquitin ligase Cereblon door Pomalidomide-based homo-PROTACs
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Chemische inactivatie van de E3 Ubiquitin ligase Cereblon door Pomalidomide-based homo-PROTACs

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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Dit werk beschrijft de synthese en karakterisering van een op pomalidomide gebaseerde, bifunctionele homo-PROTAC als een nieuwe benadering voor het induceren van alomtegenwoordige en afbraak van de E3 ubiquitine ligase cereblon (CRBN), het doelwit van thalidomide analogen.

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Chemie afgifte 147 crbn protac imid pomalidomide ubiquitine ligase multipel myeloom proteasoom
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