Discovery of TUG-770

Elisabeth Christiansen; Steffen Vissing Fahnøe Hansen; Christian Urban; Brian D Hudson; Edward T Wargent; Manuel Grundmann; Laura Jenkins; Mohamed Zaibi; Claire J Stocker; Susanne Ullrich; Evi Kostenis; Matthias U Kassack; Graeme Milligan; Michael A Cawthorne; Trond Ulven

doi:10.1021/ml4000673

Discovery of TUG-770

Elisabeth Christiansen, Steffen Vissing Fahnøe Hansen, Christian Urban, Brian D Hudson, Edward T Wargent, Manuel Grundmann, Laura Jenkins, Mohamed Zaibi, Claire J Stocker, Susanne Ullrich, Evi Kostenis, Matthias U Kassack, Graeme Milligan, Michael A Cawthorne, Trond Ulven

52 Citations (Scopus)

Abstract

Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.

Original language	English
Journal	A C S Medicinal Chemistry Letters
Volume	4
Issue number	5
Pages (from-to)	441-445
Number of pages	5
ISSN	1948-5875
DOIs	https://doi.org/10.1021/ml4000673
Publication status	Published - 9 May 2013
Externally published	Yes

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10.1021/ml4000673

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title = "Discovery of TUG-770",

abstract = "Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.",

author = "Elisabeth Christiansen and Hansen, {Steffen Vissing Fahn{\o}e} and Christian Urban and Hudson, {Brian D} and Wargent, {Edward T} and Manuel Grundmann and Laura Jenkins and Mohamed Zaibi and Stocker, {Claire J} and Susanne Ullrich and Evi Kostenis and Kassack, {Matthias U} and Graeme Milligan and Cawthorne, {Michael A} and Trond Ulven",

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T1 - Discovery of TUG-770

AU - Christiansen, Elisabeth

AU - Hansen, Steffen Vissing Fahnøe

AU - Urban, Christian

AU - Hudson, Brian D

AU - Wargent, Edward T

AU - Grundmann, Manuel

AU - Jenkins, Laura

AU - Zaibi, Mohamed

AU - Stocker, Claire J

AU - Ullrich, Susanne

AU - Kostenis, Evi

AU - Kassack, Matthias U

AU - Milligan, Graeme

AU - Cawthorne, Michael A

AU - Ulven, Trond

PY - 2013/5/9

Y1 - 2013/5/9

N2 - Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.

AB - Free fatty acid receptor 1 (FFA1 or GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and currently attracts high interest as a new target for the treatment of type 2 diabetes. We here report the discovery of a highly potent FFA1 agonist with favorable physicochemical and pharmacokinetic properties. The compound efficiently normalizes glucose tolerance in diet-induced obese mice, an effect that is fully sustained after 29 days of chronic dosing.

U2 - 10.1021/ml4000673

DO - 10.1021/ml4000673

M3 - Journal article

SN - 1948-5875

VL - 4

SP - 441

EP - 445

JO - A C S Medicinal Chemistry Letters

JF - A C S Medicinal Chemistry Letters

IS - 5

ER -

Discovery of TUG-770

Abstract

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