Variable path length and counter-flow continuous variation methods for the study of the formation of high-affinity complexes by absorbance spectroscopy. An application to the studies of substrate binding in cytochrome P450

Biophys Chem. 2006 Sep 20;123(2-3):95-101. doi: 10.1016/j.bpc.2006.04.007. Epub 2006 Apr 26.

Abstract

Studies of the equilibrium of protein-ligand interactions and determination of the stoichiometry of protein complexes constitute an important element of routine biochemical practice. In this paper we describe two innovative modifications of Job's method of continuous variation, which allow us to analyze tight interactions and determine stoichiometry in multi-site binding systems, including cases where the absorbance of the ligand overlaps with that of the enzyme-ligand complex. Our results on the interactions of cytochromes P450 3A4 and P450eryF with substrates illustrate the applicability of these approaches to the studies of substrate binding in enzymes that exhibit homotropic cooperativity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Binding Sites
  • Bromocriptine / chemistry*
  • Cytochrome P-450 Enzyme System / biosynthesis
  • Cytochrome P-450 Enzyme System / chemistry*
  • Equipment Design
  • Ligands
  • Methylamines / chemistry*
  • Pyrenes / chemistry*
  • Sensitivity and Specificity
  • Spectrum Analysis / methods
  • Structure-Activity Relationship
  • Substrate Specificity
  • Titrimetry

Substances

  • 1-pyrenemethylamine
  • Ligands
  • Methylamines
  • Pyrenes
  • Bromocriptine
  • Cytochrome P-450 Enzyme System