Kinetic characterization of fragment binding in AmpC β-lactamase by high-throughput molecular simulations

J Chem Inf Model. 2014 Feb 24;54(2):362-6. doi: 10.1021/ci4006063. Epub 2014 Jan 30.

Abstract

Small molecules used in fragment-based drug discovery form multiple, promiscuous binding complexes difficult to capture experimentally. Here, we identify such binding poses and their associated energetics and kinetics using molecular dynamics simulations on AmpC β-lactamase. Only one of the crystallographic binding poses was found to be thermodynamically favorable; however, the ligand shows several binding poses within the pocket. This study demonstrates free-binding molecular simulations in the context of fragment-to-lead development and its potential application in drug design.

Publication types

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

MeSH terms

  • Bacterial Proteins / chemistry
  • Bacterial Proteins / metabolism*
  • Drug Evaluation, Preclinical
  • Escherichia coli / enzymology
  • High-Throughput Screening Assays*
  • Kinetics
  • Molecular Dynamics Simulation*
  • Protein Binding
  • Protein Conformation
  • Small Molecule Libraries / metabolism*
  • Thermodynamics
  • Thiophenes / metabolism
  • beta-Lactamases / chemistry
  • beta-Lactamases / metabolism*

Substances

  • Bacterial Proteins
  • Small Molecule Libraries
  • Thiophenes
  • AmpC beta-lactamases
  • beta-Lactamases