Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370139 | Bioorganic & Medicinal Chemistry Letters | 2011 | 7 Pages |
Abstract
GPR119 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. During a programme aimed at developing agonists of the GPR119 receptor, we identified compounds that were potent with reduced hERG liabilities, that had good pharmacokinetic properties and that displayed excellent glucose-lowering effects in vivo. However, further profiling in a GPR119 knock-out (KO) mouse model revealed that the biological effects were not exclusively due to GPR119 agonism, highlighting the value of transgenic animals in drug discovery programs.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Katy J. Brocklehurst, Anders Broo, Roger J. Butlin, Hayley S. Brown, David S. Clarke, Öjvind Davidsson, Kristin Goldberg, Sam D. Groombridge, Elizabeth E. Kelly, Andrew Leach, Darren McKerrecher, Charles O’Donnell, Simon Poucher, Paul Schofield,