Catalytic in vivo protein knockdown by small-molecule PROTACs Daniel P Bondeson , Alina Mares , Ian E D Smith , Eunhwa Ko , Sebastien Campos , Afjal H Miah , Katie E Mulholland , Natasha Routly , Dennis L Buckley , Jeffrey L Gustafson , Nico Zinn , Paola Grandi , Satoko Shimamura , Giovanna Bergamini , Maria Faelth-Savitski , Marcus Bantscheff , Carly Cox , Deborah A Gordon , Ryan R Willard , John J Flanagan , Linda N Casillas , Bartholomew J Votta , Willem den Besten , Kristoffer Famm , Laurens Kruidenier , Paul S Carter , John D Harling , Ian Churcher , Craig M Crews Nature Chemical Biology（2015）
摘要
The use of a high-affinity VHL ligand allows the development of chimeric molecules that promote the association of ERRα or RIPK2 with the VHL E3 ubiquitin ligase complex, resulting in protein degradation.
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pharmacology, proteomics, small molecules
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