Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

Elisabeth Christiansen; Maria E Due-Hansen; Christian Urban; Manuel Grundmann; Ralf Schröder; Brian D Hudson; Graeme Milligan; Michael A Cawthorne; Evi Kostenis; Matthias U Kassack; Trond Ulven

doi:10.1021/jm3002026

Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

Elisabeth Christiansen, Maria E Due-Hansen, Christian Urban, Manuel Grundmann, Ralf Schröder, Brian D Hudson, Graeme Milligan, Michael A Cawthorne, Evi Kostenis, Matthias U Kassack, Trond Ulven

45 Citationer (Scopus)

Abstract

FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.

Originalsprog	Engelsk
Tidsskrift	Journal of Medicinal Chemistry
Vol/bind	55
Udgave nummer	14
Sider (fra-til)	6624-6628
Antal sider	5
ISSN	0022-2623
DOI	https://doi.org/10.1021/jm3002026
Status	Udgivet - 2012
Udgivet eksternt	Ja

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10.1021/jm3002026

Citationsformater

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title = "Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists",

abstract = "FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.",

author = "Elisabeth Christiansen and Due-Hansen, {Maria E} and Christian Urban and Manuel Grundmann and Ralf Schr{\"o}der and Hudson, {Brian D} and Graeme Milligan and Cawthorne, {Michael A} and Evi Kostenis and Kassack, {Matthias U} and Trond Ulven",

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doi = "10.1021/jm3002026",

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volume = "55",

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journal = "Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

AU - Christiansen, Elisabeth

AU - Due-Hansen, Maria E

AU - Urban, Christian

AU - Grundmann, Manuel

AU - Schröder, Ralf

AU - Hudson, Brian D

AU - Milligan, Graeme

AU - Cawthorne, Michael A

AU - Kostenis, Evi

AU - Kassack, Matthias U

AU - Ulven, Trond

PY - 2012

Y1 - 2012

N2 - FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.

AB - FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage on 5. The appendage significantly lowers lipophilicity and improves metabolic stability while preserving potency, resulting in discovery of the potent FFA1 agonist 13.

U2 - 10.1021/jm3002026

DO - 10.1021/jm3002026

M3 - Journal article

SN - 0022-2623

VL - 55

SP - 6624

EP - 6628

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 14

ER -

Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists

Abstract

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