{Reference Type}: Journal Article
{Title}: A native chemical ligation handle that enables the synthesis of advanced activity-based probes: diubiquitin as a case study.
{Author}: Mulder MP;El Oualid F;ter Beek J;Ovaa H;
{Journal}: Chembiochem
{Volume}: 15
{Issue}: 7
{Year}: May 2014 5
{Factor}: 3.461
{DOI}: 10.1002/cbic.201402012
{Abstract}: We present the development of a native chemical ligation handle that also functions as a masked electrophile that can be liberated during synthesis when required. This handle can thus be used for the synthesis of complex activity-based probes. We describe the use of this handle in the generation of linkage-specific activity-based deubiquitylating enzyme probes that contain substrate context and closely mimic the native ubiquitin isopeptide linkage. We have generated activity-based probes based on all seven isopeptide-linked diubiquitin topoisomers and demonstrated their structural integrity and ability to label DUBs in a linkage-specific manner.