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JoVE Journal Chemistry
Inativação química da E3 ubiquitina ligase Cereblon por Homo-PROTACs à base de Pomalidomida
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Inativação química da E3 ubiquitina ligase Cereblon por Homo-PROTACs à base de Pomalidomida

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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Este trabalho descreve a síntese e caracterização de um Homo-PROTAC bifuncional, com base em pomalidomida, como uma nova abordagem para induzir a ubiquitinação e a degradação do E3 ubiquitina ligase Cereblon (CRBN), alvo de análogos da talidomida.

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Química crbn ProTac Imid pomalidomida ubiquitina ligase mieloma múltiplo Proteassoma
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