Interactions between beta-lactam antibiotics and isolated membranes of Streptococcus faecalis ATCC 9790

Eur J Biochem. 1977 May 2;75(1):231-9. doi: 10.1111/j.1432-1033.1977.tb11522.x.

Abstract

The DD-carboxypeptidase-exchange membrane-bound enzyme in Streptococcus faecalis ATCC 9790 reacts with beta-lactam antibiotics to form complexes with rather long half-lives. Depending upon the antibiotic, the second-order rate constants for complex formation range from 0.75-560 M-1 S-1 (at 37 degrees C and in water) and the first-order rate constants for complex breakdown range from 1.3 to 26 x 10(-5) s-1 (at 37 degrees C and in 5 mM phosphate buffer pH 7.5). There are about 30 pmol of DD-carboxypeptidase-exchange enzyme per mg of membrane protein. The degradation products arising from benzylpenicillin are phenylacetylglycine and probably N-formyl-D-penicillamine. Isolated membranes also contain other penicillin binding sites (about 70 pmol/mg membrane protein). That part of benzylpenicillin which reacts with at least some of these latter sites is slowly degraded into penicilloic acid. Normal functioning of the DD-carboxypeptidase-exchange membrane-bound enzyme is important, if not essential, for cell growth. With the beta-lactam antibiotics tested inhibition of cell growth is mainly related to the rates of formation of the inactive enzyme-antibiotic complexes. The relationship, however, is not a direct one probably due to the competitive effect exerted by the other penicillin binding sites.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Binding Sites
  • Carboxypeptidases / metabolism*
  • Cell Membrane / enzymology*
  • Enterococcus faecalis / enzymology*
  • Kinetics
  • Muramoylpentapeptide Carboxypeptidase / metabolism*
  • Penicillin G / analogs & derivatives
  • Penicillin G / metabolism*
  • Penicillins / metabolism*
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Penicillins
  • Carboxypeptidases
  • Muramoylpentapeptide Carboxypeptidase
  • Penicillin G