Origins of the activity of PAL and LAP enzyme inhibitors: toward ab initio binding affinity prediction

J Am Chem Soc. 2005 Feb 16;127(6):1658-9. doi: 10.1021/ja042691v.

Abstract

Interaction energies of phenylalanine ammonia-lyase (PAL) active site residues with a series of PAL inhibitors have been partitioned into electrostatic, exchange, delocalization, and correlation components and compared with analogous results obtained previously for leucine aminopeptidase (LAP). In the latter metalloenzyme, either of the two charged residues controls entirely relative inhibitor binding energies, while at least four residues are required to determine ligand relative stabilization in neutral PAL. Significant correlation with experimental inhibitory activity was found between the stabilization energy at gradually decreasing levels of theory (MP2, SCF) down to the first-order Heitler-London term. Contrary to the LAP case, where the electrostatic term was sufficient to reproduce experimentally observed trends, in the case of PAL, exchange repulsion effects also have to be considered. Computational protocol presented herein constitutes a promising way to incorporate the first principle calculation's accuracy into the process of rational binding affinity prediction, revealing the physical nature of the interactions, where successive approximations can be introduced in a systematic and justifiable manner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Cattle
  • Crystallins / antagonists & inhibitors
  • Crystallins / chemistry
  • Crystallins / metabolism
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology
  • Kinetics
  • Leucyl Aminopeptidase / antagonists & inhibitors*
  • Leucyl Aminopeptidase / chemistry
  • Leucyl Aminopeptidase / metabolism
  • Phenylalanine Ammonia-Lyase / antagonists & inhibitors*
  • Phenylalanine Ammonia-Lyase / chemistry
  • Phenylalanine Ammonia-Lyase / metabolism
  • Plant Proteins / antagonists & inhibitors
  • Plant Proteins / chemistry
  • Plant Proteins / metabolism
  • Thermodynamics

Substances

  • Crystallins
  • Enzyme Inhibitors
  • Plant Proteins
  • Leucyl Aminopeptidase
  • Phenylalanine Ammonia-Lyase