Soluble epoxide hydrolase, a target with multiple opportunities for cardiovascular drug discovery.
Soluble epoxide hydrolase (sEH) is a cross-functional target, with the potential for therapeutic utility in the areas of hypertension, inflammation, and organ-protection. Promising target validation has emerged around soluble epoxide hydrolase in recent years which suggests that small molecule inhibitors may have utility in cardio protection, glucose regulation, hypertension, inflammation, and organ protection. Based on the diversity of chemical classes of sEH inhibitors reported in the literature, there exists a real opportunity to definitively determine the best therapeutic utility for an sEH inhibitor. Recent advances in target validation and tool compounds from medicinal chemistry efforts will be described.
Marino
Joseph P
JP
Metabolic Pathways Center of Excellence in Drug Discovery, GlaxoSmithKline Research and Development, King of Prussia, PA 19406, USA. joseph.p.marino@gsk.com
D000818:Animals; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000201:enzymology; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors*; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D012995:Solubility; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D004851:Epoxide Hydrolases