Catalytic in vivo protein knockdown by small-molecule PROTACs

The current predominant theapeutic paradigm is based on maximizing drug-receptor occupancy to achieve clinical benefit. This strategy, however, generally requires excessive drug concentrations to ensure sufficient occupancy, often leading to adverse side effects. Here, we describe major improvements...

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Bibliografiske detaljer
Udgivet i:Nat Chem Biol
Main Authors: Bondeson, Daniel P, Mares, Alina, Smith, Ian E D, Ko, Eunhwa, Campos, Sebastien, Miah, Afjal H, Mulholland, Katie E, Routly, Natasha, Buckley, Dennis L, Gustafson, Jeffrey L, Zinn, Nico, Grandi, Paola, Shimamura, Satoko, Bergamini, Giovanna, Faelth-Savitski, Maria, Bantscheff, Marcus, Cox, Carly, Gordon, Deborah A, Willard, Ryan R, Flanagan, John J, Casillas, Linda N, Votta, Bartholomew J, den Besten, Willem, Famm, Kristoffer, Kruidenier, Laurens, Carter, Paul S, Harling, John D, Churcher, Ian, Crews, Craig M
Format: Artigo
Sprog:Inglês
Udgivet: 2015
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Article
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4629852/
https://ncbi.nlm.nih.gov/pubmed/26075522
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.1858
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