Macclesfield, United Kingdom
Macclesfield, United Kingdom

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Brocklehurst K.J.,Mereside | Broo A.,Pepparedsleden 1 | Butlin R.J.,Mereside | Brown H.S.,Mereside | And 14 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

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. © 2011 Elsevier Ltd. All rights reserved.


PubMed | Mereside
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2011

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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