Stable Phosphohistidine Analogues by Click Chemistry

Protein phosphorylation has been a hot spot in both academic and industrial research for possible drug targets. Instability and isomerism of Phosphohistidine however presents great difficulties in such studies.


Now a stable version of PhosphoHistidine has been developed using click chemistry by Muir and coworkers from The Rockefeller UniVersity and Active Motif, Inc.
JACS 2010, 14327. Published on Web 9/29/2010.


See "Active Motif offers click chemistry reagents" Tuesday, October 5, 2010


The preparation uses the two regio-selective click chemistries, Cu1+ and Ru2+ catalyses, for two stable isomers. They succesfully used these stable analogues in SPPS (solid phase peptide synthesis) to synthesize peptides. Also succesful was the development of the first antibody specifically for pHis.


Two small, good-looking molecules out of click chemistry!