A highly selective probe for human cytochrome P450 3A4: isoform selectivity, kinetic characterization and its applications

Chem Commun (Camb). 2013 Oct 28;49(84):9779-81. doi: 10.1039/c3cc45250f.

Abstract

Bufalin 5β-hydroxylation was found to be an isoform-specific biotransformation probe substrate for cytochrome P450 3A4 (CYP3A4). The probe reaction was well-characterized and it can be used for measuring the real catalytic activities of CYP3A4 from different enzyme sources.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biocatalysis
  • Bufanolides / chemistry
  • Bufanolides / metabolism*
  • Cytochrome P-450 CYP3A / chemistry
  • Cytochrome P-450 CYP3A / metabolism*
  • Humans
  • Hydroxylation
  • Isoenzymes / chemistry
  • Isoenzymes / metabolism
  • Kinetics
  • Models, Molecular
  • Molecular Conformation
  • Molecular Probes / chemistry
  • Molecular Probes / metabolism*

Substances

  • Bufanolides
  • Isoenzymes
  • Molecular Probes
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human
  • bufalin