Design of soluble epoxide hydrolase inhibitors as drug leads

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Presentation transcript:

Design of soluble epoxide hydrolase inhibitors as drug leads Junghwa Kim, Elise Pellmann, Mike Wild Daniel Sem, Ph.D. John Imig, Ph.D.

sEH: biology Epoxyeicosatrienoic acids (EETs) Cytochrome P450 Vasodilation, anti-inflammatory, angiogenesis sEH inhibition

sEH: biochemistry Two domains: hydrolase (N-terminal), phosphatase (C-terminal)

sEH As a Teaching Example Hydrolysis of Epoxides, Enzyme Activity, Catalytic Triad

Imig Group Experiment Development of EET Analogs Studied Male Rats Renal Effects Blood Pressure/Heart Rate Most Promising Lead- 11,12-ether-EET-8-ZE

Inhibitor Design Study of 1VJ5 Crystal Structure Propose Drug Leads Jmol and Swiss Viewer Propose Drug Leads Draw in ChemDraw From Swiss Viewer

Inhibitor Design Draw Structure of Drugs in Spartan Place designed drugs on Enzyme (sEH) through Discovery Studio Visualizer

What’s next? Kinetic assays (in vitro): Determine Kd, mode of inhibition ADMET (in vivo, in silico) In silico: docking, TOPKAT (accelrys)