作者:Oleksandr Koniev、Geoffray Leriche、Marc Nothisen、Jean-Serge Remy、Jean-Marc Strub、Christine Schaeffer-Reiss、Alain Van Dorsselaer、Rachid Baati、Alain Wagner
DOI:10.1021/bc400469d
日期:2014.2.19
Exquisite chemoselectivity for cysteine has been found for a novel class of remarkably hydrolytically stable reagents, 3-arylpropiolonitriles (APN). The efficacy of the APN-mediated tagging was benchmarked against other cysteine-selective methodologies in a model study on a series of traceable amino acid derivatives. The selectivity of the methodology was further explored on peptide mixtures obtained by trypsin digestion of lysozyme. Additionally, the superior stability of APN-cysteine conjugates in aqueous media, human plasma, and living cells makes this new thiol-click reaction a promising methodology for applications in bioconjugation.