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Agonists/antagonists/enzyme inhibitors Agonists/antagonists/enzyme inhibitors
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Genomics Genomics
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Proteomics Proteomics
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Metabolomics Metabolomics
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Further reading Further reading
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1.2 Targeted drug discovery: receptor-based approaches
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Published:May 2013
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Agonists/antagonists/enzyme inhibitors
Agonist, antagonist, and enzyme inhibitor approaches are all employed in drug discovery, with genomics, metabolomics, and proteomics helping to deliver potential targets.
The systemic effects of agonists or antagonists may also be further studied with knockout animal approaches. The Cre IoxP approach works by introducing IoxP sequences of DNA either side of the target gene. Cre-recombinase can then be used to remove the target gene in a knockout animal, and a similar approach used to introduce extra genes in a knock in animal.
Where hepatic enzyme agonism or antagonism is the goal, sophisticated in vitro systems now exist for testing the effect of drug targets. In vitro models of gut membrane transport have also been developed for absorption studies.
Genomics
Genomics-based approaches to drug discovery centre on evaluating differences in gene expression in the diseased versus the healthy state. These lead to identification of one or usually a number of genes, which when expressed or not expressed lead to changes in the functional status of the individual.
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