Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.

@article{Lizarzaburu2012DiscoveryAO,
  title={Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.},
  author={Mike E. Lizarzaburu and Simon Turcotte and Xiaohui Du and Jason Duquette and Angela Fu and Jonathan B. Houze and LePing Li and Junfeng Liu and Michiko Murakoshi and Kozo Oda and Ryo Okuyama and Futoshi Nara and Jeff D. Reagan and Ming Yu and Julio C. Medina},
  journal={Bioorganic & medicinal chemistry letters},
  year={2012},
  volume={22 18},
  pages={
          5942-7
        }
}
The discovery and initial optimization of a series of phenylalanine based agonists for GPR142 is described. The structure-activity-relationship around the major areas of the molecule was explored to give agonists 90 times more potent than the initial HTS hit in a human GPR142 inositol phosphate accumulation assay. Removal of CYP inhibition by exploration of the pyridine A-ring is also described. 
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Discovery and pharmacological effects of a novel GPR142 antagonist.

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  • 2017
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