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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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Bibliografski detalji
Izdano u:Chem Sci
Glavni autori: 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
Jezik:Inglês
Izdano: Royal Society of Chemistry 2016
Teme:
Online pristup: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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