Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy. / Hansen, Steffen Vissing Fahnøe; Christiansen, Elisabeth; Urban, Christian; Hudson, Brian D; Stocker, Claire J; Due-Hansen, Maria E; Wargent, Ed T; Shimpukade, Bharat; Almeida, Reinaldo; Ejsing, Christer S; Cawthorne, Michael A; Kassack, Matthias U; Milligan, Graeme; Ulven, Trond.

In: Journal of Medicinal Chemistry, Vol. 59, No. 6, 01.03.2016, p. 2841-2846.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Hansen, SVF, Christiansen, E, Urban, C, Hudson, BD, Stocker, CJ, Due-Hansen, ME, Wargent, ET, Shimpukade, B, Almeida, R, Ejsing, CS, Cawthorne, MA, Kassack, MU, Milligan, G & Ulven, T 2016, 'Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy', Journal of Medicinal Chemistry, vol. 59, no. 6, pp. 2841-2846. https://doi.org/10.1021/acs.jmedchem.5b01962

APA

Hansen, S. V. F., Christiansen, E., Urban, C., Hudson, B. D., Stocker, C. J., Due-Hansen, M. E., Wargent, E. T., Shimpukade, B., Almeida, R., Ejsing, C. S., Cawthorne, M. A., Kassack, M. U., Milligan, G., & Ulven, T. (2016). Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy. Journal of Medicinal Chemistry, 59(6), 2841-2846. https://doi.org/10.1021/acs.jmedchem.5b01962

Vancouver

Hansen SVF, Christiansen E, Urban C, Hudson BD, Stocker CJ, Due-Hansen ME et al. Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy. Journal of Medicinal Chemistry. 2016 Mar 1;59(6):2841-2846. https://doi.org/10.1021/acs.jmedchem.5b01962

Author

Hansen, Steffen Vissing Fahnøe ; Christiansen, Elisabeth ; Urban, Christian ; Hudson, Brian D ; Stocker, Claire J ; Due-Hansen, Maria E ; Wargent, Ed T ; Shimpukade, Bharat ; Almeida, Reinaldo ; Ejsing, Christer S ; Cawthorne, Michael A ; Kassack, Matthias U ; Milligan, Graeme ; Ulven, Trond. / Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy. In: Journal of Medicinal Chemistry. 2016 ; Vol. 59, No. 6. pp. 2841-2846.

Bibtex

@article{334346ded34740af91e1f2a2eddad331,
title = "Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy",
abstract = "The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.",
author = "Hansen, {Steffen Vissing Fahn{\o}e} and Elisabeth Christiansen and Christian Urban and Hudson, {Brian D} and Stocker, {Claire J} and Due-Hansen, {Maria E} and Wargent, {Ed T} and Bharat Shimpukade and Reinaldo Almeida and Ejsing, {Christer S} and Cawthorne, {Michael A} and Kassack, {Matthias U} and Graeme Milligan and Trond Ulven",
year = "2016",
month = mar,
day = "1",
doi = "10.1021/acs.jmedchem.5b01962",
language = "English",
volume = "59",
pages = "2841--2846",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "6",

}

RIS

TY - JOUR

T1 - Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy

AU - Hansen, Steffen Vissing Fahnøe

AU - Christiansen, Elisabeth

AU - Urban, Christian

AU - Hudson, Brian D

AU - Stocker, Claire J

AU - Due-Hansen, Maria E

AU - Wargent, Ed T

AU - Shimpukade, Bharat

AU - Almeida, Reinaldo

AU - Ejsing, Christer S

AU - Cawthorne, Michael A

AU - Kassack, Matthias U

AU - Milligan, Graeme

AU - Ulven, Trond

PY - 2016/3/1

Y1 - 2016/3/1

N2 - The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.

AB - The free fatty acid receptor 1 (FFA1 or GPR40) is established as an interesting potential target for treatment of type 2 diabetes. However, to obtain optimal ligands, it may be necessary to limit both lipophilicity and polar surface area, translating to a need for small compounds. We here describe the identification of 24, a potent FFA1 agonist with low lipophilicity and very high ligand efficiency that exhibit robust glucose lowering effect.

U2 - 10.1021/acs.jmedchem.5b01962

DO - 10.1021/acs.jmedchem.5b01962

M3 - Journal article

VL - 59

SP - 2841

EP - 2846

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 6

ER -

ID: 189161642