Minimalist synthetic host with stacked guanidinium ions mimics the weakened hydration shells of protein-protein interaction interfaces

J Org Chem. 2014 Jan 3;79(1):34-40. doi: 10.1021/jo401949s. Epub 2013 Dec 18.

Abstract

Protein surfaces are complex solutes, and protein-protein interactions are specifically mediated by surface motifs that modulate solvation shells in poorly understood ways. We report herein a supramolecular host that is designed to mimic one of the most important recognition motifs that drives protein-protein interactions, the stacked arginine side chain. We show that it binds its guests and displays good selectivity in the highly competitive medium of pure, buffered water. We use a combination of experimental studies of binding and molecular dynamics simulations to build a cohesive picture of how this biomimetic host achieves the feat. The presence of the stacking element next to the guanidinium groups causes a decrease in the number of host-water hydrogen bonds, a decrease in the density of water around the host, and a decrease in water-water hydrogen bonds near the host. Experimental data using mixed organic/aqueous solvent systems confirm that this host relies on the hydrophobic effect in a way that the two control hosts do not. Our simulations and analysis provide detailed information on the linkage between (de)hydration and binding events in water in a way that could be applied to many aqueous supramolecular systems.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Guanidine / chemistry*
  • Hydrogen Bonding
  • Hydrophobic and Hydrophilic Interactions
  • Ions / chemistry*
  • Protein Interaction Domains and Motifs
  • Solvents / chemistry*
  • Water / chemistry*

Substances

  • Ions
  • Solvents
  • Water
  • Guanidine