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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Detalhes bibliográficos
Publicado no:J Am Chem Soc
Main Authors: 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
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha: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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