Soluble Epoxide Hydrolase as a Therapeutic Target for Cardiovascular Diseases
By J. Imig, Bruce D. Hammock. Nature reviews. Drug discovery, 2009
625 citations recorded by the source corpus.
The cardiovascular effects of epoxyeicosatrienoic acids (EETs) include vasodilation, antimigratory actions on vascular smooth muscle cells and anti-inflammatory actions. These endogenous lipid mediators are broken down into diols by soluble epoxide hydrolase (sEH), and so inhibiting this enzyme would be expected to enhance the beneficial cardiovascular properties of EETs. sEH inhibitors (sEHIs) that are based on 1,3-disubstituted urea have been rapidly developed, and have been shown to be antihypertensive and anti-inflammatory, and to protect the brain, heart and kidney from damage. Although challenges for the future exist — including improving the drug-like properties of sEHIs and finding better ways to target sEHIs to specific tissues — the recent initiation of the first clinical trials of sEHIs has highlighted the therapeutic potential of these agents.
Subfields: Biochemistry, Endocrinology, Diabetes and Metabolism, Organic Chemistry
View Paper: https://www.semanticscholar.org/paper/3d83dac4d095820a50ad502818c4dc4fe8040241
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In Biochemistry
In Endocrinology, Diabetes and Metabolism
In Organic Chemistry
Citations in the corpus
- The influence of lipophilicity in drug discovery and design (2012, methodology): “The application of LE and LLE in drug optimization is highlighted by several recent examples, including the design of a potent cyclin-dependent kinase 2 (CDK2) inhibitor [24,25], protein kinase B inhibitor [26], soluble epoxide hydrolase inhibitors [27], CB2 agonists [28], CB2 agonists/CB1 agonists ”