Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. / Christiansen, Elisabeth; Urban, Christian; Grundmann, Manuel; Due-Hansen, Maria Elisabeth; Hagesaether, Ellen; Schmidt, Johannes; Pardo, Leonardo; Ullrich, Susanne; Kostenis, Evi; Kassack, Matthias U; Ulven, Trond.

In: Journal of Medicinal Chemistry, Vol. 54, No. 19, 2011, p. 6691-6703.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Christiansen, E, Urban, C, Grundmann, M, Due-Hansen, ME, Hagesaether, E, Schmidt, J, Pardo, L, Ullrich, S, Kostenis, E, Kassack, MU & Ulven, T 2011, 'Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties', Journal of Medicinal Chemistry, vol. 54, no. 19, pp. 6691-6703. https://doi.org/10.1021/jm2005699

APA

Christiansen, E., Urban, C., Grundmann, M., Due-Hansen, M. E., Hagesaether, E., Schmidt, J., Pardo, L., Ullrich, S., Kostenis, E., Kassack, M. U., & Ulven, T. (2011). Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. Journal of Medicinal Chemistry, 54(19), 6691-6703. https://doi.org/10.1021/jm2005699

Vancouver

Christiansen E, Urban C, Grundmann M, Due-Hansen ME, Hagesaether E, Schmidt J et al. Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. Journal of Medicinal Chemistry. 2011;54(19):6691-6703. https://doi.org/10.1021/jm2005699

Author

Christiansen, Elisabeth ; Urban, Christian ; Grundmann, Manuel ; Due-Hansen, Maria Elisabeth ; Hagesaether, Ellen ; Schmidt, Johannes ; Pardo, Leonardo ; Ullrich, Susanne ; Kostenis, Evi ; Kassack, Matthias U ; Ulven, Trond. / Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. In: Journal of Medicinal Chemistry. 2011 ; Vol. 54, No. 19. pp. 6691-6703.

Bibtex

@article{a3a46a3458e34c7fbea912738d4ad294,
title = "Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties",
abstract = "The free fatty acid receptor 1 (FFA1, also known as GPR40) enhances glucose-stimulated insulin secretion from pancreatic {\ss}-cells and is recognized as an interesting new target for treatment of type 2 diabetes. Several series of selective FFA1 agonists are already known. Most of these are derived from free fatty acids (FFAs) or glitazones, and are relatively lipophilic. Aiming at the development of potent, selective and less lipophilic FFA1 agonists, the terminal phenyl of a known compound series was replaced by nitrogen containing heterocycles. This resulted in the identification of 37, a selective FFA1 agonist with potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E, optimal lipophilicity and excellent in vitro permeability and metabolic stability.",
author = "Elisabeth Christiansen and Christian Urban and Manuel Grundmann and Due-Hansen, {Maria Elisabeth} and Ellen Hagesaether and Johannes Schmidt and Leonardo Pardo and Susanne Ullrich and Evi Kostenis and Kassack, {Matthias U} and Trond Ulven",
year = "2011",
doi = "10.1021/jm2005699",
language = "English",
volume = "54",
pages = "6691--6703",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "19",

}

RIS

TY - JOUR

T1 - Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties

AU - Christiansen, Elisabeth

AU - Urban, Christian

AU - Grundmann, Manuel

AU - Due-Hansen, Maria Elisabeth

AU - Hagesaether, Ellen

AU - Schmidt, Johannes

AU - Pardo, Leonardo

AU - Ullrich, Susanne

AU - Kostenis, Evi

AU - Kassack, Matthias U

AU - Ulven, Trond

PY - 2011

Y1 - 2011

N2 - The free fatty acid receptor 1 (FFA1, also known as GPR40) enhances glucose-stimulated insulin secretion from pancreatic ß-cells and is recognized as an interesting new target for treatment of type 2 diabetes. Several series of selective FFA1 agonists are already known. Most of these are derived from free fatty acids (FFAs) or glitazones, and are relatively lipophilic. Aiming at the development of potent, selective and less lipophilic FFA1 agonists, the terminal phenyl of a known compound series was replaced by nitrogen containing heterocycles. This resulted in the identification of 37, a selective FFA1 agonist with potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E, optimal lipophilicity and excellent in vitro permeability and metabolic stability.

AB - The free fatty acid receptor 1 (FFA1, also known as GPR40) enhances glucose-stimulated insulin secretion from pancreatic ß-cells and is recognized as an interesting new target for treatment of type 2 diabetes. Several series of selective FFA1 agonists are already known. Most of these are derived from free fatty acids (FFAs) or glitazones, and are relatively lipophilic. Aiming at the development of potent, selective and less lipophilic FFA1 agonists, the terminal phenyl of a known compound series was replaced by nitrogen containing heterocycles. This resulted in the identification of 37, a selective FFA1 agonist with potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E, optimal lipophilicity and excellent in vitro permeability and metabolic stability.

U2 - 10.1021/jm2005699

DO - 10.1021/jm2005699

M3 - Journal article

VL - 54

SP - 6691

EP - 6703

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 19

ER -

ID: 189162096