ENZYME-INHIBITION IN OPEN SYSTEMS - SUPERIORITY OF UNCOMPETITIVE AGENTS

Investigations of the open system behavior of reversible dead-end inhi bitors were carried out by means of computer simulations and experimen tal studies. The results from both approaches indicate that substrate- competitive inhibition may often be an inappropriate basis for design of potential therapeutic agents. The use of uncompetitive (also called anticompetitive) inhibitors in this role is likely to be far more eff ective. Chemical analogs of pathogen-specific enzymic reaction product s rather than analogs of substrates provide a promising basis for the systematic design of such uncompetitive inhibitors.