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Journal / Chemistry / Inactivation chimique de l'E3 Ubiquitin Ligase…
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JoVE Journal Chemistry
Inactivation chimique de l'E3 Ubiquitin Ligase Cereblon par des Homo-PROTAC à base de Pomalidomide
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Inactivation chimique de l'E3 Ubiquitin Ligase Cereblon par des Homo-PROTAC à base de Pomalidomide

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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Ce travail décrit la synthèse et la caractérisation d'un homo-PROTAC bifonctionnel à base de pomalidomide comme une nouvelle approche pour induire l'ubiquitination et la dégradation du cereblon de ligase d'ubiquitine E3 (CRBN), la cible des analogues de la thalidomide.

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Chimie Numéro 147 CRBN PROTAC IMiD pomalidomide ubiquitine ligase myélome multiple protéasome
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