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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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Vydáno v:Chem Sci
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: Royal Society of Chemistry 2016
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On-line přístup: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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