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A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Research into the chemical biology of bromodomains has been driven by the development of acetyl-lysine mimetics. The ligands are typically anchored by binding to a highly conserved asparagine residue. Atypical bromodomains, for which the asparagine is mutated, have thus far proven elusive targets, i...

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Détails bibliographiques
Publié dans:Chem Sci
Auteurs principaux: Cox, Oakley B., Krojer, Tobias, Collins, Patrick, Monteiro, Octovia, Talon, Romain, Bradley, Anthony, Fedorov, Oleg, Amin, Jahangir, Marsden, Brian D., Spencer, John, von Delft, Frank, Brennan, Paul E.
Format: Artigo
Langue:Inglês
Publié: Royal Society of Chemistry 2016
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Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5977933/
https://ncbi.nlm.nih.gov/pubmed/29910922
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1039/c5sc03115j
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