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Competitive inhibitors are commonly used to make pharmaceuticals. [3] For example, methotrexate is a chemotherapy drug that acts as a competitive inhibitor. It is structurally similar to the coenzyme, folate, which binds to the enzyme dihydrofolate reductase. [3]
For example, an inhibitor might compete with substrate A for the first binding site, but be a non-competitive inhibitor with respect to substrate B in the second binding site. [ 26 ] Traditionally reversible enzyme inhibitors have been classified as competitive, uncompetitive, or non-competitive, according to their effects on K m and V max . [ 14 ]
Dapagliflozin is an example of an SGLT-2 inhibitor, it is a competitive, highly selective inhibitor of SGLT. It acts via selective and potent inhibition of SGLT-2, and its activity is based on each patient's underlying blood sugar control and kidney function. The results are decreased kidney reabsorption of glucose, glucosuria effect increases ...
Enzyme induction is a process in which a molecule (e.g. a drug) induces (i.e. initiates or enhances) the expression of an enzyme. Enzyme inhibition can refer to the inhibition of the expression of the enzyme by another molecule; interference at the enzyme-level, basically with how the enzyme works.
In response to decreased tetrahydrofolate (THF), the cell begins to transcribe more DHF reductase, the enzyme that reduces DHF to THF. Because methotrexate is a competitive inhibitor of DHF reductase, increased concentrations of DHF reductase can overcome the drugs inhibition. Many new drugs are under development to reduce antifolate drug ...
Non-depolarizing blockers are reversed by acetylcholinesterase inhibitor drugs since non-depolarizing blockers are competitive antagonists at the ACh receptor so can be reversed by increases in ACh. The depolarizing blockers already have ACh-like actions, so these agents have prolonged effect under the influence of acetylcholinesterase inhibitors.
Examples of this drug class are atorvastatin, rosuvastatin, fluvastatin, simvastatin, pravastatin and lovastatin. Most efficacious in lowering LDL-C levels, statins block the action of HMG-CoA reductase through competitive inhibition. [18]
This is a favorable drug design over many clinically used competing agents, because most of them, such as clavulanic acid, become hydrolysed, and are therefore only useful for a finite period of time. This generally causes the need for a higher concentration of competitive inhibitor than would be necessary in an unhydrolyzable inhibitor.