Search results
Results from the WOW.Com Content Network
Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies. [2]Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50%, respectively.
In contrast to irreversible inhibitors, reversible inhibitors generally do not undergo chemical reactions when bound to the enzyme and can be easily removed by dilution or dialysis. A special case is covalent reversible inhibitors that form a chemical bond with the enzyme, but the bond can be cleaved so the inhibition is fully reversible.
Most competitive inhibitors function by binding reversibly to the active site of the enzyme. [1] As a result, many sources state that this is the defining feature of competitive inhibitors. [ 7 ] This, however, is a misleading oversimplification , as there are many possible mechanisms by which an enzyme may bind either the inhibitor or the ...
Jänne PA, Gray N, Settleman J (September 2009). "Factors underlying sensitivity of cancers to small-molecule kinase inhibitors". Nature Reviews. Drug Discovery. 8 (9): 709– 23. doi:10.1038/nrd2871. PMID 19629074. S2CID 7817325. Roskoski R (March 2021). "Properties of FDA-approved small molecule protein kinase inhibitors: A 2021 update".
Uncompetitive inhibition is present within biological systems in a number of ways. In fact, it often becomes clear that the traits of inhibition specific to uncompetitive inhibitors, such as their tendency to act at their best at high concentrations of substrate, are essential to some important bodily functions operating properly. [7]
All PI3K inhibitors that are currently approved inhibit one or more p110 isoforms of the class I PI3Ks. Inhibiting different p110 isoforms can have different effects, [15] e.g. PTEN-negative tumors may be more sensitive to PIK3CB inhibitors. [15]
Integrated liquid-liquid extraction can be used to remove products that have a density that differs from the rest of the bioreactors contents. [8] This is done by adding a solvent downstream of the bioreactor and letting the product separate out in a settling tank before the bioreactor effluent is moved to a secondary reactor or returned to its initial reactor to continue its cultivation.
An inhibitor can reduce the effectiveness of a catalyst in a catalysed reaction (either a non-biological catalyst or an enzyme).E.g., if a compound is so similar to (one of) the reactants that it can bind to the active site of a catalyst but does not undergo a catalytic reaction then that catalyst molecule cannot perform its job because the active site is occupied.