Conformation control of abiotic α-helical foldamers

J Chem Inf Model. 2013 Oct 28;53(10):2671-80. doi: 10.1021/ci400365y. Epub 2013 Oct 11.

Abstract

With the aim to find new protein-protein inhibitors, a three part methodology was applied to oligophenylpyridines. Theoretical ring twist angle predictions have been validated by X-ray diffraction and molecular dynamics simulations with NMR constraints. Careful choice of substituent and nitrogen positions in oligophenylpyridyl foldamer units opens the way to conformational control of the side chain distribution of this α-helix mimic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Circular Dichroism
  • Crystallography, X-Ray
  • Hydrogen Bonding
  • Molecular Conformation
  • Molecular Dynamics Simulation
  • Molecular Mimicry
  • Proteins / chemistry*
  • Pyridines / chemistry*
  • Small Molecule Libraries / chemistry*
  • Structure-Activity Relationship
  • Thermodynamics

Substances

  • Proteins
  • Pyridines
  • Small Molecule Libraries