Synergistic inhibition of aminopeptidase B by penicillamine or cysteine and metallic salts.
The inhibition of aminopeptidase B by D- and L-penicillamine and D- and L-cysteine is reported. All these alpha-amino-beta-mercapto acids inhibit moderately this enzyme, with IC50 values in the 10(-4) range. This inhibition was not reversed by Zn2+ ions, but a synergistic effect was observed. A similar effect took place by the combined use of D-penicillamine and Fe2+, Ca2+ or Ni2+ salts, but not with copper salts. The zinc-D-penicillamine and zinc-D-cysteine complexes 3 and 4 show an inhibitory potency approximately 5-fold higher than that of the corresponding amino acid.
Herranz
R
R
Instituto de Química Médica, C.S.I.C., Madrid, Spain.
García-López
M T
MT
Pérez
C
C
D000626:Aminopeptidases / Q000037:antagonists & inhibitors*; D000818:Animals; D003545:Cysteine / Q000494:pharmacology*; D004357:Drug Synergism; D066298:In Vitro Techniques; D007739:L Cells; D008670:Metals / Q000494:pharmacology*; D051379:Mice; D010396:Penicillamine / Q000494:pharmacology*
D008670:Metals; D000626:Aminopeptidases; C019721:aminopeptidase B; D010396:Penicillamine; D003545:Cysteine