1359969-39-3Relevant articles and documents
New β-strand templates constrained by Huisgen cycloaddition
Pehere, Ashok D.,Abell, Andrew D.
, p. 1330 - 1333 (2012/05/20)
New peptidic templates constrained into a β-strand geometry by linking acetylene and azide containing P1 and P3 residues of a tripeptide by Huisgen cycloaddition are presented. The conformations of the macrocycles are defined by NMR studies and those that best define a β-strand are shown to be potent inhibitors of the protease calpain. The β-strand templates presented and defined here are prepared under optimized conditions that should be suitable for targeting a range of proteases and other applications requiring such a geometry.