Lessons in PROTAC design from selective degradation with a promiscuous warhead

Inhibiting protein function selectively is a major goal of modern drug discovery. Here, we report a previously understudied benefit of small molecule Proteolysis Targeting Chimera (PROTACs) that recruit E3 ubiquitin ligases to target proteins for their ubiquitination and subsequent proteasome-mediat...

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Gepubliceerd in:Cell Chem Biol
Hoofdauteurs: Bondeson, Daniel P, Smith, Blake E, Burslem, George M, Buhimschi, Alexandru D, Hines, John, Jaime-Figueroa, Saul, Wang, Jing, Hamman, Brian D, Ishchenko, Alexey, Crews, Craig M
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2017
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Article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5777153/
https://ncbi.nlm.nih.gov/pubmed/29129718
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.chembiol.2017.09.010
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