This document, titled "Enzyme inhibitors for drug discovery," discusses the value of enzymes as therapeutic targets for drug development. The article highlights the potential of enzyme inhibition in various fields, including oncology, viral/parasitic diseases, bacterial infections, metabolic dysfunctions, ...
and the process involved is termed enzyme inhibition.Some enzyme inhibitors are normal body metabolites that inhibit a particular enzyme while other inhibitors may be foreign substances, such as drugs or toxins. The inhibition
This was the first drug approved in the USA for therapy in Alzheimer's disease. Despite moderate success, its use was subsequently discontinued because of adverse effects. Along with several other cholinesterase inhibitors, it has also been marketed as a cognitive enhancing (nootropic) agent. ...
Examples of drugs that are irreversible enzyme inhibitors are shown in Table 2.4. Table 2.4. Examples of Irreversible Enzyme Inhibitor Drugs DrugStructureTarget Nexium H+/K+ ATPase in gastric parietal cells Allopurinol Xanthine oxidase Ibrutinib Bruton’s tyrosine kinase 5-Fluorouracil Thymidylate ...
Assessment of Enzyme Inhibition: A Review with Examples from the Development of Monoamine Oxidase and Cholinesterase Inhibitory Drugs 来自 EBSCO 喜欢 0 阅读量: 55 作者:R Rona,T Keith 摘要: The actions of many drugs involve enzyme inhibition. This is exemplified by the inhibitors of monoamine ...
53). Other examples of drugs that are enzyme inhibitors are shown inTable 10.5. To make life even more difficult, several inhibitors of drug metabolism influence the metabolism of different stereoisomers selectively. Examples of drugs that inhibit the metabolism of the active (S) and less active...
The significance of enzymes as targets of drug action is discussed. New approaches to the rational design of enzyme inhibitors are characterized by a pronounced shift of emphasis toward the targets of drug action, as the structure and function of an increasing number of enzymes are described in ...
The angiotensin converting enzyme (ACE) inhibitors are a group of effective drugs with a unique mechanism of action. These drugs have proven to be useful f
The FabI inhibitors have been divided into two groups, based on whether they form a covalent adduct with the NAD+ cofactor. Inhibitors that form a covalent adduct include the diazaborines, as well as the front-line tuberculosis drug isoniazid. The NAD adducts formed with these compounds are ...
Role of CYPs in Human Drug Metabolism P450Percentage of Total Hepatic CYP PoolApproximate Percentage of Drugs That are SubstratesExamples of SubstratesExamples of InhibitorsExamples of Inducers CYP1A2 15 ~5 Fluvoxamine Caffeine Cyclobenzaprine Theophylline Thiothixene Olanzapine Ciprofloxacin Fluvoxamine ...