Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 2, Pages 662-666Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.06.037
Keywords
Bioorthogonal chemistry; Cyclooctyne; Activity-based protein profiling; Proteasome inhibitor; Strain-promoted cycloaddition
Funding
- Netherlands Organisation for Scientific Research (NWO)
- Netherlands Genomics Initiative (NGI)
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The development and application of bioorthogonal two-step labeling techniques receives much attention. Employing bifunctional proteasome probe 2 the efficiency of two-step labeling of recently published biotinylated cyclooctynes 3-5 is compared to Staudinger-Bertozzi ligation in cell extracts and living cells. While cyclooctynes 3-5 react faster and at a much lower concentration then the Staudinger-Bertozzi benchmark, background labeling is considerable with these reagents. (C) 2011 Elsevier Ltd. All rights reserved.
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