Iron(IV)hydroxide pK(a) and the role of thiolate ligation in C-H bond activation by cytochrome P450

Science. 2013 Nov 15;342(6160):825-9. doi: 10.1126/science.1244373.

Abstract

Cytochrome P450 enzymes activate oxygen at heme iron centers to oxidize relatively inert substrate carbon-hydrogen bonds. Cysteine thiolate coordination to iron is posited to increase the pK(a) (where K(a) is the acid dissociation constant) of compound II, an iron(IV)hydroxide complex, correspondingly lowering the one-electron reduction potential of compound I, the active catalytic intermediate, and decreasing the driving force for deleterious auto-oxidation of tyrosine and tryptophan residues in the enzyme's framework. Here, we report on the preparation of an iron(IV)hydroxide complex in a P450 enzyme (CYP158) in ≥90% yield. Using rapid mixing technologies in conjunction with Mössbauer, ultraviolet/visible, and x-ray absorption spectroscopies, we determine a pK(a) value for this compound of 11.9. Marcus theory analysis indicates that this elevated pK(a) results in a >10,000-fold reduction in the rate constant for oxidations of the protein framework, making these processes noncompetitive with substrate oxidation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Carbon / chemistry
  • Catalysis
  • Cysteine / analogs & derivatives*
  • Cysteine / chemistry
  • Cytochrome P-450 Enzyme System / chemistry*
  • Enzyme Activation
  • Hydrogen Bonding
  • Hydroxides / chemistry*
  • Oxidation-Reduction
  • Tryptophan / chemistry
  • Tyrosine / chemistry

Substances

  • Hydroxides
  • cysteine thiolate
  • Tyrosine
  • Carbon
  • Tryptophan
  • Cytochrome P-450 Enzyme System
  • hydroxide ion
  • Cysteine