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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Publicat a:J Am Chem Soc
Autors principals: 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
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2019
Accés en línia: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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