Toward Computational Understanding of Molecular Recognition in the Human Metabolizing Cytochrome P450s

Curr Med Chem. 2018;25(28):3353-3373. doi: 10.2174/0929867325666180226104126.

Abstract

Cytochrome P450s are enzymes capable of metabolizing a wide variety of drugs. Their significant impact in drug discovery has led to extensive research, computationally and experimentally, in order to explore how a chemical entity responds to metabolizing enzymes. We present an overview of ligand-based and structure-based methodologies, along with pertinent information on the structures, biology, and relevance of these enzymes.

Keywords: 3D-QSAR; Cytochrome P450; crystal structures; docking; drug metabolism; molecular dynamics; sites of metabolism..

Publication types

  • Review

MeSH terms

  • Binding Sites
  • Cytochrome P-450 Enzyme System / metabolism*
  • Humans
  • Ligands
  • Molecular Docking Simulation
  • Pharmaceutical Preparations / chemistry
  • Pharmaceutical Preparations / metabolism*
  • Quantitative Structure-Activity Relationship

Substances

  • Ligands
  • Pharmaceutical Preparations
  • Cytochrome P-450 Enzyme System