Concepedia

Discovery of a GPR40 Superagonist: The Impact of Aryl Propionic Acid α-Fluorination

Hui Huang, Sanath K. Meegalla, James C. Lanter, Michael P. Winters, Shuyuan Zhao, James Littrell, Jenson Qi, Brian Rady, Paul S. Lee, Jianying Liu,

ACS Medicinal Chemistry Letters · 2018 · 25 citations · 20 references

DOIFull text

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Concepts

Abstract

is not only highly efficacious in lowering glucose and body weight in rodent models but also has a low DILI risk due to its stable acylglucuronide metabolite.

References

20

From the Triumvirate to the Ominous Octet: A New Paradigm for the Treatment of Type 2 Diabetes Mellitus

Ralph A. DeFronzo · Diabetes · 2009 · 3K citations · Full text

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<i>Gpr40</i> Is Expressed in Enteroendocrine Cells and Mediates Free Fatty Acid Stimulation of Incretin Secretion

Sara Edfalk, Pär Steneberg, Helena Edlund · Diabetes · 2008 · 571 citations · Full text

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Relationship between daily dose of oral medications and idiosyncratic drug-induced liver injury: Search for signals

Craig Lammert, Stefán Einarsson, Chandan Saha et al. · Hepatology · 2008 · 388 citations · Full text

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High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875

Ankita Srivastava, Jason K. Yano, Yoshihiko Hirozane et al. · Nature · 2014 · 344 citations

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TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial

Charles Burant, Prabhakar Viswanathan, John Marcinak et al. · The Lancet · 2012 · 245 citations

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