title: Basic models for differential inhibition of enzymes.
abstract: The possible preferential action exerted by an inhibitor on the transformation of one of two agonist substrates catalyzed by the same enzyme has recently been reported in studies on aldose reductase inhibition. This event was defined as "intra-site differential inhibition" and the molecules able to exert this action as "differential inhibitors". This work presents some basic kinetic models describing differential inhibition. Using a simple analytic approach, the results show that differential inhibition can occur through either competitive or mixed type inhibition in which the inhibitor prevalently targets the free enzyme. The results may help in selecting molecules whose differential inhibitory action could be advantageous in controlling the activity of enzymes acting on more than one substrate.
authors: Department of Biology, University of Pisa, Via S. Zeno, 51, Pisa 56127, Italy.
authors: Mario
authors: M
authors: Cappiello
authors: Department of Biology, University of Pisa, Via S. Zeno, 51, Pisa 56127, Italy.
authors: Roberta
authors: R
authors: Moschini
authors: Department of Biology, University of Pisa, Via S. Zeno, 51, Pisa 56127, Italy.
authors: Francesco
authors: F
authors: Balestri
authors: Department of Biology, University of Pisa, Via S. Zeno, 51, Pisa 56127, Italy.
authors: Umberto
authors: U
authors: Mura
authors: Department of Biology, University of Pisa, Via S. Zeno, 51, Pisa 56127, Italy. Electronic address: adelcorso@biologia.unipi.it.
authors: Antonella
authors: A
authors: Del-Corso
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008954:Models, Biological; D013379:Substrate Specificity / Q000187:drug effects
chemical_list: D004791:Enzyme Inhibitors; D000449:Aldehyde Reductase
keywords: Aldose reductase; Competing substrates; Differential inhibition; Enzyme inhibition