Effect of zinc ion on the inhibition of carboxypeptidase A by imidazole-bearing substrate analogues.
Competitive inhibitors of carboxypeptidase A, 2-(4-imidazoyl)hydrocinnamic acid (1) and its congeners (2-4) that bear an imidazole ring as the zinc-ligating functionality have been evaluated for their CPA inhibitory activity in the presence of zinc ion to find that the zinc ion augments the inhibitory potency by up to 212-fold.
Han
M S
MS
Department of Chemistry and Center for Integrated Molecular Systems, Division of Molecular Life Sciences, Pohang University of Science and Technology, San 31 Hyojadong, 790-784, Pohang, Republic of Korea.
Kim
D H
DH
D001667:Binding, Competitive; D002268:Carboxypeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D043422:Carboxypeptidases A; D002934:Cinnamates / Q000737:chemistry / Q000494:pharmacology*; D004357:Drug Synergism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D013379:Substrate Specificity; D015032:Zinc / Q000494:pharmacology*
C433942:2-(4-imidazoyl)hydrocinnamic acid; D002934:Cinnamates; D004791:Enzyme Inhibitors; D007093:Imidazoles; C029899:imidazole; D002268:Carboxypeptidases; D043422:Carboxypeptidases A; D015032:Zinc