70274-57-6Relevant academic research and scientific papers
Mixing of peptides and electrophilic traps gives rise to potent, broad-spectrum proteasome inhibitors
Verdoes, Martijn,Florea, Bogdan I.,Van Der Linden, Wouter A.,Renou, Didier,Van Den Nieuwendijk, Adrianus M. C. H.,Van Der Marel, Gijs A.,Overkleeft, Herman S.
, p. 1416 - 1426 (2008/02/07)
The synthesis and evaluation of hybrid proteasome inhibitors that contain structural elements of the known inhibitors bortezomib, epoxomicin and peptide vinyl sulfones is described. From the panel of 15 inhibitors some structure activity relationships can be deduced with regard to inhibitory activity in relation to peptide recognition element, inhibitor size and nature of the electrophilic trap. Further, the panel contains one of the most potent peptide-based pan-proteasome inhibitors reported to date. This journal is The Royal Society of Chemistry.
