Versatile Platform for the Synthesis of Orthogonally Cleavable Heteromultifunctional Cross-Linkers

Bioconjug Chem. 2017 Apr 19;28(4):907-912. doi: 10.1021/acs.bioconjchem.7b00033. Epub 2017 Feb 17.

Abstract

Cleavable and heteromultifunctional cross-linkers have proven critical in a wide range of biological applications. Traditional approaches for synthesizing these linkers suffer from various synthetic and functional limitations. In this work, an efficient sequence-defined synthetic methodology, developed for the assembly of oligothioetheramides, was used to address many of these limitations. Four heterotrifunctional cross-linkers with up to two orthogonal internal cleavage sites were synthesized. These linkers were conjugated to a pair of fluorophores that undergo Förster resonance energy transfer (FRET) and a model protein-human transferrin. Orthogonal bond cleavage was validated by mass spectrometry, fluorescent gel electrophoresis, and confocal microscopy. These studies demonstrate the versatility and biological utility of oligothioetheramides as a new class of multifunctional chemical cross-linkers and biologically relevant fluorescent probes.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry*
  • Boron Compounds / chemistry
  • Cross-Linking Reagents / chemical synthesis
  • Cross-Linking Reagents / chemistry*
  • Ethers / chemical synthesis
  • Ethers / chemistry
  • Fluorescence Resonance Energy Transfer
  • Fluorescent Dyes / chemistry*
  • HeLa Cells
  • Humans
  • Microscopy, Confocal
  • Models, Molecular
  • Transferrin / chemistry*

Substances

  • 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
  • Amides
  • Boron Compounds
  • Cross-Linking Reagents
  • Ethers
  • Fluorescent Dyes
  • Transferrin