Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

[Image: see text] The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker. Here we examined the impact of derivatizing two different BET bromodomain...

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Detalles Bibliográficos
Autores principales: Chan, Kwok-Ho, Zengerle, Michael, Testa, Andrea, Ciulli, Alessio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5788402/
https://www.ncbi.nlm.nih.gov/pubmed/28595007
http://dx.doi.org/10.1021/acs.jmedchem.6b01912

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5788402/
https://www.ncbi.nlm.nih.gov/pubmed/28595007
http://dx.doi.org/10.1021/acs.jmedchem.6b01912

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