Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening

[Image: see text] Covalent probes can display unmatched potency, selectivity, and duration of action; however, their discovery is challenging. In principle, fragments that can irreversibly bind their target can overcome the low affinity that limits reversible fragment screening, but such electrophil...

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Publicado en:J Am Chem Soc
Autores principales: Resnick, Efrat, Bradley, Anthony, Gan, Jinrui, Douangamath, Alice, Krojer, Tobias, Sethi, Ritika, Geurink, Paul P., Aimon, Anthony, Amitai, Gabriel, Bellini, Dom, Bennett, James, Fairhead, Michael, Fedorov, Oleg, Gabizon, Ronen, Gan, Jin, Guo, Jingxu, Plotnikov, Alexander, Reznik, Nava, Ruda, Gian Filippo, Díaz-Sáez, Laura, Straub, Verena M., Szommer, Tamas, Velupillai, Srikannathasan, Zaidman, Daniel, Zhang, Yanling, Coker, Alun R., Dowson, Christopher G., Barr, Haim M., Wang, Chu, Huber, Kilian V.M., Brennan, Paul E., Ovaa, Huib, von Delft, Frank, London, Nir
Formato: Artigo
Lenguaje:Inglês
Publicado: American Chemical Society 2019
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC6556873/
https://ncbi.nlm.nih.gov/pubmed/31060360
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jacs.9b02822
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