competitive inhibitor


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com·pet·i·tive in·hi·bi·tion

blocking of the action of an enzyme by a compound that binds to the free enzyme, preventing the substrate from binding and thus preventing the enzyme from acting on that substrate. The competitive inhibitor is often a substrate analogue and binds at the active site; however, this is not an absolute requirement for competitive inhibition. Saturating concentrations of substrate can remove the inhibition. Compare: isostery.

competitive inhibitor

an inhibitor of an enzyme reaction that competes with the substrate by binding at the active site.

competitive inhibitor

1. A chemical that binds to or blocks another reagent from participating in a reaction.
2. A medication, hormone, or other intercellular messenger that binds and blocks the cellular receptor or target enzyme of another agent. Drugs that act by competitive inhibition may treat or prevent disease by inactivating pathogenic enzymes or by blocking the effects of hormones or precursor molecules. For example, protease inhibitors interfere with production of human immunodeficiency virus (HIV) by binding and inactivating the protease enzyme; selective estrogen-receptor modulators limit the impact of estrogen by replacing this hormone on cells sensitive to its effects.
See also: inhibitor
References in periodicals archive ?
The data in this study demonstrate that the MA was not only a weak competitive inhibitor of CYP3A4 in humans, but also a weak competitive inhibitor of CYP2C11 and 3A2 in rats, with [K.
It is clear from the in vitro inhibition kinetic studies in pooled human liver microsomes that cryptotanshinone and dihydrotanshinone can act as competitive inhibitors to human CYP2C9 which is mainly responsible for tolbutamide 4-hydroxylation.
The heterocyclical molecules called tiadizolidinones (TDZDs), of whose family proceeds the NP031112 molecule, represents the first non-ATP competitive inhibitors of GSK3 described so far and have been proposed as new effective drugs for the treatment of neurodegenerative disorders, where the hyperphosphorylation of the tau protein plays a leading role, as in the case of Alzheimer's.
Hirsutism that is associated with hyperandrogenism often can be lessened by drugs that are competitive inhibitors of the androgen receptor.
One key differentiator of BNC420 is that it displays significant selectivity to VEGFR3 over related VEGFR receptors, while other competitive inhibitors of the VEGFR receptors (e.
The new dimerization inhibitor unveils a biologically meaningful rationale for suppressing angiogenesis in tumors that could outperform traditional competitive inhibitors of angiogenesis in tumor therapy.
While the previous generation of p38 MAPK inhibitors suffered from side effects such as liver transaminase elevations, the newer inhibitors are more selective at targeting p38 and include non-ATP competitive inhibitors directed against the conformation epitope.
The Report discusses strategies to design peptidomimetic and non-peptidomimetic competitive inhibitors, as well as other types of inhibitors.

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