AMA_Role_of_Enzyme_Structure_function_and_Regulation_in_Drug_Discovery_Programme.docx

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Importance of understanding enzyme’s structure, function and regulation in modern drug discovery Name Course Professor Date
Enzyme role in Drug Discovery 2 Importance of understanding enzyme’s structure, function and regulation in modern drug discovery Introduction A Recent trend in medicine has been marked by the development of molecular science. Copeland explains that special interests have been directed in targeting particular macromolecules that are associated with a disease or has pathogenic bioactivity 1 . Enzymes are some of the prevalent biomolecules with continued exploitation in the development of drugs. Enzymes have been associated with diseases processes, inhibition, and metabolism of drugs. Drug development can exploit such association. Moreover, enzymes have been exploited as drug targets 2 . Drug metabolism is also a critical issue in understanding pharmacokinetics such as therapeutic effects, side effects, and interindividual differences 3 . This article seeks to evaluate the role of enzymes in the discovery of drugs. In achieving this, the article explores the role enzymes play in drug development. The article considers three aspects concerned with enzymes in their application in the discovery of new drugs. First, the article evaluates reasons for the use of enzymes as drug targets. Such application of enzymes reflects the role of structure in drug discovery and development 1 . As earlier mentioned, drug metabolism is of critical importance in drug discovery. Moreover, the paper performs an exploration of the role of drug metabolism in their developmentis also done. Such an exploration is pertinent in explaining how enzyme function and inhibition plays role in drug discovery. Role of enzymes in drug discovery: The importance of structure, function and regulation Enzymes are the primary molecules involved in catalysis 1 . The enzymes are composed of polypeptide chains that have a regular structural pattern. The structural scaffolding of an enzyme
Enzyme role in Drug Discovery 3 provides a spatial orientation that facilitates a specific catalysis reaction. Such specificity of the spatial configuration and prevalence of enzymes in catalytic reactions can be used as a drug target. For a drug to be effective, it is expected to exhibit some physicochemical properties. Such involve, be able to be absorbed, able to permeate cell membrane, be distributed and maintained in the body for some considerate amount of time. These properties are formulated in consideration to the enzyme involved in the disease processes involved. Specificity of the drugs to a particular enzyme requires understating of the active site of an enzyme and hence their structural scaffolding. For instance, dihydrofolate reductase enzyme is involved in the

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