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Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor

The recently discovered apelin/APJ system has emerged as a critical mediator of cardiovascular homeostasis and is associated with the pathogenesis of cardiovascular disease. A role for apelin/APJ in energy metabolism and gastrointestinal function has also recently emerged. We disclose the discovery...

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Bibliographic Details
Main Authors: Maloney, Patrick R., Khan, Pasha, Hedrick, Michael, Gosalia, Palak, Milewski, Monika, Li, Linda, Roth, Gregory P., Sergienko, Eduard, Suyama, Eigo, Sugarman, Eliot, Nguyen, Kevin, Mehta, Alka, Vasile, Stefan, Su, Ying, Stonich, Derek, Nguyen, Hung, Zeng, Fu-Yue, Mangravita Novo, Arianna, Vicchiarelli, Michael, Diwan, Jena, Chung, Thomas D. Y., Smith, Layton H., Pinkerton, Anthony B.
Format: Artigo
Language:Inglês
Published: 2012
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC3729231/
https://ncbi.nlm.nih.gov/pubmed/23010269
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.08.105
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