Assembling Ligands In Situ Using Bioorthogonal Boronate Ester Synthesis

作者:Shin Sung Bin Y; Almeida Ramiro D; Gerona Navarro Guillermo; Bracken Clay; Jaffrey Samie R*
来源:Chemistry & Biology, 2010, 17(11): 1171-1176.
DOI:10.1016/j.chembiol.2010.09.008

摘要

Many molecules that could manipulate cellular function are not practical due to their large size and concomitant undesirable pharmocokinetic properties. Here, we describe a bioorthogonal, highly stable boronate ester (HiSBE) synthesis and use this reaction to synthesize a biologically active molecule from smaller precursors in a physiological context. The rapid rate of HiSBE synthesis suggests that it may be useful for assembling a wide variety of biologically active molecules in physiological solutions.

  • 出版日期2010-11-24