Deuteration as a General Strategy to Enhance Azobenzene-Based Photopharmacology

Angew Chem Int Ed Engl. 2024 Sep 23;63(39):e202408300. doi: 10.1002/anie.202408300. Epub 2024 Aug 19.

Abstract

Chemical photoswitches have become a widely used approach for the remote control of biological functions with spatiotemporal precision. Several molecular scaffolds have been implemented to improve photoswitch characteristics, ranging from the nature of the photoswitch itself (e.g. azobenzenes, dithienylethenes, hemithioindigo) to fine-tuning of aromatic units and substituents. Herein, we present deuterated azobenzene photoswitches as a general means of enhancing the performance of photopharmacological molecules. Deuteration can improve azobenzene performance in terms of light sensitivity (higher molar extinction coefficient), photoswitch efficiency (higher photoisomerization quantum yield), and photoswitch kinetics (faster macroscopic rate of photoisomerization) with minimal alteration to the underlying structure of the photopharmacological ligand. We report synthesized deuterated azobenzene-based ligands for the optimized optical control of ion channel and G protein-coupled receptor (GPCR) function in live cells, setting the stage for the straightforward, widespread adoption of this approach.

Keywords: Azobenzene; Deuteration; G Protein-Coupled Receptor; Ion Channel; Photopharmacology.

MeSH terms

  • Azo Compounds* / chemical synthesis
  • Azo Compounds* / chemistry
  • Deuterium* / chemistry
  • Humans
  • Ion Channels / chemistry
  • Ion Channels / metabolism
  • Ligands
  • Light
  • Molecular Structure
  • Photochemical Processes
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / metabolism

Substances

  • Azo Compounds
  • azobenzene
  • Deuterium
  • Ligands
  • Receptors, G-Protein-Coupled
  • Ion Channels