|
|||||
|
|
Palladium‐Catalyzed Chemoselective and Biocompatible Functionalization of Cysteine‐Containing Molecules at Room Temperature |
|
| Authors: | Riyadh Ahmed Atto Al‐Shuaeeb Dr Sergii Kolodych Dr Oleksandr Koniev Dr Sébastien Delacroix Stéphane Erb Stéphanie Nicolaÿ Dr Jean‐Christophe Cintrat Prof Jean‐Daniel Brion Dr Sarah Cianférani Dr Mouâd Alami Dr Alain Wagner Dr Samir Messaoudi |
| Institution: | 1. BioCIS, Equipe Labellisée Ligue Contre le Cancer, Univ. Paris-Sud, CNRS, University Paris-Saclay, Chatenay-Malabry, France;2. Syndivia SAS, Illkirch, France;3. BioOrganic Mass Spectrometry Laboratory (LSMBO), IPHC, University of Strasbourg, Strasbourg, France;4. IPHC, CNRS, UMR7178, Strasbourg, France;5. SAMM, US 31 INSERM—UMS 3679 CNRS, University Paris-Saclay, Chatenay-Malabry, France;6. IBITECS—Laboratoire de Chimie Bioorganique, CEA-Saclay, Saclay, France;7. Laboratory of Functional Chemo Systems, LabEx MEDALIS, Faculté de Pharmacie, Strasbourg, France |
| Abstract: | The third generation of aminobiphenyl palladacycle pre‐catalyst “G3‐Xantphos” enables functionalization of peptides containing cysteine in high yields. The conjugation (bioconjugation) occurs chemoselectively at room temperature under biocompatible conditions. Extension of the method to protein functionalization allows selective bioconjugation of the trastuzumab antibody. |
| Keywords: | amino acids antibody– drug conjugates bioconjugation C− S bond-forming reaction palladium catalysis peptides |