Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

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

Standard

Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. / Hansen, Anders Højgaard; Christensen, Henriette B.; Pandey, Sunil K.; Sergeev, Eugenia; Valentini, Alice; Dunlop, Julia; Dedeo, Domonkos; Fratta, Simone; Hudson, Brian D.; Milligan, Graeme; Ulven, Trond; Ulven, Elisabeth Rexen.

In: ChemMedChem, Vol. 16, No. 21, 2021, p. 3326-3341.

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

Harvard

Hansen, AH, Christensen, HB, Pandey, SK, Sergeev, E, Valentini, A, Dunlop, J, Dedeo, D, Fratta, S, Hudson, BD, Milligan, G, Ulven, T & Ulven, ER 2021, 'Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2', ChemMedChem, vol. 16, no. 21, pp. 3326-3341. https://doi.org/10.1002/cmdc.202100356

APA

Hansen, A. H., Christensen, H. B., Pandey, S. K., Sergeev, E., Valentini, A., Dunlop, J., Dedeo, D., Fratta, S., Hudson, B. D., Milligan, G., Ulven, T., & Ulven, E. R. (2021). Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. ChemMedChem, 16(21), 3326-3341. https://doi.org/10.1002/cmdc.202100356

Vancouver

Hansen AH, Christensen HB, Pandey SK, Sergeev E, Valentini A, Dunlop J et al. Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. ChemMedChem. 2021;16(21):3326-3341. https://doi.org/10.1002/cmdc.202100356

Author

Hansen, Anders Højgaard ; Christensen, Henriette B. ; Pandey, Sunil K. ; Sergeev, Eugenia ; Valentini, Alice ; Dunlop, Julia ; Dedeo, Domonkos ; Fratta, Simone ; Hudson, Brian D. ; Milligan, Graeme ; Ulven, Trond ; Ulven, Elisabeth Rexen. / Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. In: ChemMedChem. 2021 ; Vol. 16, No. 21. pp. 3326-3341.

Bibtex

@article{aa12883ae5ce45ec91937bb0dd2b4b18,
title = "Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2",
abstract = "Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.",
keywords = "FFA2, GPCR, GPR43, inflammation, short-chain fatty acids",
author = "Hansen, {Anders H{\o}jgaard} and Christensen, {Henriette B.} and Pandey, {Sunil K.} and Eugenia Sergeev and Alice Valentini and Julia Dunlop and Domonkos Dedeo and Simone Fratta and Hudson, {Brian D.} and Graeme Milligan and Trond Ulven and Ulven, {Elisabeth Rexen}",
year = "2021",
doi = "10.1002/cmdc.202100356",
language = "English",
volume = "16",
pages = "3326--3341",
journal = "Farmaco",
issn = "1860-7179",
publisher = "Wiley - V C H Verlag GmbH & Co. KGaA",
number = "21",

}

RIS

TY - JOUR

T1 - Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

AU - Hansen, Anders Højgaard

AU - Christensen, Henriette B.

AU - Pandey, Sunil K.

AU - Sergeev, Eugenia

AU - Valentini, Alice

AU - Dunlop, Julia

AU - Dedeo, Domonkos

AU - Fratta, Simone

AU - Hudson, Brian D.

AU - Milligan, Graeme

AU - Ulven, Trond

AU - Ulven, Elisabeth Rexen

PY - 2021

Y1 - 2021

N2 - Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.

AB - Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.

KW - FFA2

KW - GPCR

KW - GPR43

KW - inflammation

KW - short-chain fatty acids

U2 - 10.1002/cmdc.202100356

DO - 10.1002/cmdc.202100356

M3 - Journal article

C2 - 34288488

VL - 16

SP - 3326

EP - 3341

JO - Farmaco

JF - Farmaco

SN - 1860-7179

IS - 21

ER -

ID: 276322295