Crystallographic and kinetic studies of human mitochondrial acetoacetyl-CoA thiolase: the importance of potassium and chloride ions for its structure and function

Biochemistry. 2007 Apr 10;46(14):4305-21. doi: 10.1021/bi6026192. Epub 2007 Mar 20.

Abstract

Thiolases are CoA-dependent enzymes which catalyze the formation of a carbon-carbon bond in a Claisen condensation step and its reverse reaction via a thiolytic degradation mechanism. Mitochondrial acetoacetyl-coenzyme A (CoA) thiolase (T2) is important in the pathways for the synthesis and degradation of ketone bodies as well as for the degradation of 2-methylacetoacetyl-CoA. Human T2 deficiency has been identified in more than 60 patients. A unique property of T2 is its activation by potassium ions. High-resolution human T2 crystal structures are reported for the apo form and the CoA complex, with and without a bound potassium ion. The potassium ion is bound near the CoA binding site and the catalytic site. Binding of the potassium ion at this low-affinity binding site causes the rigidification of a CoA binding loop and an active site loop. Unexpectedly, a high-affinity binding site for a chloride ion has also been identified. The chloride ion is copurified, and its binding site is at the dimer interface, near two catalytic loops. A unique property of T2 is its ability to use 2-methyl-branched acetoacetyl-CoA as a substrate, whereas the other structurally characterized thiolases cannot utilize the 2-methylated compounds. The kinetic measurements show that T2 can degrade acetoacetyl-CoA and 2-methylacetoacetyl-CoA with similar catalytic efficiencies. For both substrates, the turnover numbers increase approximately 3-fold when the potassium ion concentration is increased from 0 to 40 mM KCl. The structural analysis of the active site of T2 indicates that the Phe325-Pro326 dipeptide near the catalytic cavity is responsible for the exclusive 2-methyl-branched substrate specificity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetyl-CoA C-Acetyltransferase / chemistry*
  • Acetyl-CoA C-Acetyltransferase / genetics
  • Acetyl-CoA C-Acetyltransferase / isolation & purification
  • Acetyl-CoA C-Acetyltransferase / metabolism*
  • Acyl Coenzyme A / metabolism
  • Amino Acid Sequence
  • Apoenzymes / chemistry
  • Binding Sites
  • Catalysis
  • Chlorides / chemistry
  • Chlorides / metabolism*
  • Conserved Sequence
  • Crystallography, X-Ray
  • Dimerization
  • Dipeptides / chemistry
  • Escherichia coli / genetics
  • Humans
  • Hydrogen Bonding
  • Ions
  • Kinetics
  • Mitochondria / enzymology*
  • Models, Molecular
  • Molecular Sequence Data
  • Phenylalanine / chemistry
  • Potassium / chemistry
  • Potassium / metabolism*
  • Proline / chemistry
  • Protein Binding
  • Protein Structure, Quaternary
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Protein Subunits / chemistry
  • Protein Subunits / metabolism
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / isolation & purification
  • Recombinant Proteins / metabolism
  • Sequence Homology, Amino Acid
  • Substrate Specificity

Substances

  • Acyl Coenzyme A
  • Apoenzymes
  • Chlorides
  • Dipeptides
  • Ions
  • Protein Subunits
  • Recombinant Proteins
  • acetoacetyl CoA
  • Phenylalanine
  • 2-methylacetoacetyl-coenzyme A
  • Proline
  • Acetyl-CoA C-Acetyltransferase
  • Potassium

Associated data

  • PDB/2IB7
  • PDB/2IB8
  • PDB/2IB9
  • PDB/2IBU
  • PDB/2IBW
  • PDB/2IBY