Phenylalanine analogues as inhibitors of phenylalanine-hydroxylase from rat liver. New conclusions concerning kinetic behaviors of the enzyme

Biochimie. 1978;60(8):787-94. doi: 10.1016/s0300-9084(78)80023-6.

Abstract

The conversion of phenylalanine to tyrosine is catalysed by phenylalanine-hydroxylase. The substrate phenylalanine shows two effects: (1) allosteric transition at low phenylalanine concentrations, (2) excess substration inhibition. The molecular structure of phenylalanine-hydroxylase has not yet been elucidated. However, a tetrameric structure has been proposed. The Kinetic analysis with respect to substrate analogues suggest the existence of three types of sites on each protomer: (1) a catalytic site, (2) a non-competitive inhibitory site, (3) a positive cooperative site. Use of the enzyme's natural cofactor, tetrahydrobiopterin, has been emphasized to ensure good interpretation of the kinetic results of the phenylalanine-hydroxylase effectors.

MeSH terms

  • Allosteric Site
  • Animals
  • Binding Sites
  • Kinetics
  • Liver / enzymology*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / pharmacology
  • Phenylalanine Hydroxylase / antagonists & inhibitors*
  • Rats

Substances

  • Phenylalanine
  • Phenylalanine Hydroxylase