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Novel GPR120 agonist TUG891 modulates fat taste perception and preference and activates tongue-brain-gut axis in mice.

Murtaza B, Hichami A, Khan AS, Shimpukade B, Ulven T, Ozdener MH, Khan NA.

J Lipid Res. 2019 Dec 5. pii: jlr.RA119000142. doi: 10.1194/jlr.RA119000142. [Epub ahead of print]


An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights.

Köse M, Pillaiyar T, Namasivayam V, De Filippo E, Sylvester K, Ulven T, von Kügelgen I, Müller CE.

J Med Chem. 2019 Nov 27. doi: 10.1021/acs.jmedchem.9b01339. [Epub ahead of print]


Butyrate ameliorates allergic airway inflammation by limiting eosinophil trafficking and survival.

Theiler A, Bärnthaler T, Platzer W, Richtig G, Peinhaupt M, Rittchen S, Kargl J, Ulven T, Marsh LM, Marsche G, Schuligoi R, Sturm EM, Heinemann A.

J Allergy Clin Immunol. 2019 Sep;144(3):764-776. doi: 10.1016/j.jaci.2019.05.002. Epub 2019 May 11.


Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties.

Hansen AH, Sergeev E, Bolognini D, Sprenger RR, Ekberg JH, Ejsing CS, McKenzie CJ, Rexen Ulven E, Milligan G, Ulven T.

J Med Chem. 2018 Nov 8;61(21):9534-9550. doi: 10.1021/acs.jmedchem.8b00855. Epub 2018 Oct 12.


Dihydropyridine Fluorophores Allow for Specific Detection of Human Antibodies in Serum.

Domljanovic I, Rexen Ulven E, Ulven T, Thomsen RP, Okholm AH, Kjems J, Voss A, Taskova M, Astakhova K.

ACS Omega. 2018 Jul 31;3(7):7580-7586. doi: 10.1021/acsomega.8b00424. Epub 2018 Jul 10.


The GPR120 agonist TUG-891 promotes metabolic health by stimulating mitochondrial respiration in brown fat.

Schilperoort M, van Dam AD, Hoeke G, Shabalina IG, Okolo A, Hanyaloglu AC, Dib LH, Mol IM, Caengprasath N, Chan YW, Damak S, Miller AR, Coskun T, Shimpukade B, Ulven T, Kooijman S, Rensen PC, Christian M.

EMBO Mol Med. 2018 Mar;10(3). pii: e8047. doi: 10.15252/emmm.201708047.


Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84.

Mahmud ZA, Jenkins L, Ulven T, Labéguère F, Gosmini R, De Vos S, Hudson BD, Tikhonova IG, Milligan G.

Sci Rep. 2017 Dec 20;7(1):17953. doi: 10.1038/s41598-017-18159-3.


A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias.

Sergeev E, Hansen AH, Bolognini D, Kawakami K, Kishi T, Aoki J, Ulven T, Inoue A, Hudson BD, Milligan G.

Sci Rep. 2017 Oct 23;7(1):13741. doi: 10.1038/s41598-017-14096-3.


Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43).

Hansen AH, Sergeev E, Pandey SK, Hudson BD, Christiansen E, Milligan G, Ulven T.

J Med Chem. 2017 Jul 13;60(13):5638-5645. doi: 10.1021/acs.jmedchem.7b00338. Epub 2017 Jun 16.


Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84.

Kaspersen MH, Jenkins L, Dunlop J, Milligan G, Ulven T.

Medchemcomm. 2017 May 12;8(6):1360-1365. doi: 10.1039/c7md00130d. eCollection 2017 Jun 1.


Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation.

Dragano NRV, Solon C, Ramalho AF, de Moura RF, Razolli DS, Christiansen E, Azevedo C, Ulven T, Velloso LA.

J Neuroinflammation. 2017 Apr 26;14(1):91. doi: 10.1186/s12974-017-0869-7.


Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4.

Watterson KR, Hansen SVF, Hudson BD, Alvarez-Curto E, Raihan SZ, Azevedo CMG, Martin G, Dunlop J, Yarwood SJ, Ulven T, Milligan G.

Mol Pharmacol. 2017 Jun;91(6):630-641. doi: 10.1124/mol.116.107821. Epub 2017 Apr 6.


Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance.

Houthuijzen JM, Oosterom I, Hudson BD, Hirasawa A, Daenen LGM, McLean CM, Hansen SVF, van Jaarsveld MTM, Peeper DS, Jafari Sadatmand S, Roodhart JML, van de Lest CHA, Ulven T, Ishihara K, Milligan G, Voest EE.

FASEB J. 2017 May;31(5):2195-2209. doi: 10.1096/fj.201601248R. Epub 2017 Feb 9.


Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5).

Karlshøj S, Amarandi RM, Larsen O, Daugvilaite V, Steen A, Brvar M, Pui A, Frimurer TM, Ulven T, Rosenkilde MM.

J Biol Chem. 2016 Dec 23;291(52):26860-26874. doi: 10.1074/jbc.M116.740183. Epub 2016 Nov 10.


Pharmacological Tool Compounds for the Free Fatty Acid Receptor 4 (FFA4/GPR120).

Hansen SV, Ulven T.

Handb Exp Pharmacol. 2017;236:33-56. doi: 10.1007/164_2016_60. Review.


Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity.

Azevedo CM, Watterson KR, Wargent ET, Hansen SV, Hudson BD, Kępczyńska MA, Dunlop J, Shimpukade B, Christiansen E, Milligan G, Stocker CJ, Ulven T.

J Med Chem. 2016 Oct 13;59(19):8868-8878. Epub 2016 Sep 22.


The Neutrophil Response Induced by an Agonist for Free Fatty Acid Receptor 2 (GPR43) Is Primed by Tumor Necrosis Factor Alpha and by Receptor Uncoupling from the Cytoskeleton but Attenuated by Tissue Recruitment.

Björkman L, Mårtensson J, Winther M, Gabl M, Holdfeldt A, Uhrbom M, Bylund J, Højgaard Hansen A, Pandey SK, Ulven T, Forsman H, Dahlgren C.

Mol Cell Biol. 2016 Sep 26;36(20):2583-95. doi: 10.1128/MCB.00161-16. Print 2016 Oct 15.


Complex Pharmacology of Free Fatty Acid Receptors.

Milligan G, Shimpukade B, Ulven T, Hudson BD.

Chem Rev. 2017 Jan 11;117(1):67-110. doi: 10.1021/acs.chemrev.6b00056. Epub 2016 Jun 14. Review.


Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.

Christiansen E, Hudson BD, Hansen AH, Milligan G, Ulven T.

J Med Chem. 2016 May 26;59(10):4849-58. doi: 10.1021/acs.jmedchem.6b00202. Epub 2016 May 10.


A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor.

Grundmann M, Tikhonova IG, Hudson BD, Smith NJ, Mohr K, Ulven T, Milligan G, Kenakin T, Kostenis E.

Cell Chem Biol. 2016 Mar 17;23(3):392-403. doi: 10.1016/j.chembiol.2016.02.014.


Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice.

Gozal D, Qiao Z, Almendros I, Zheng J, Khalyfa A, Shimpukade B, Ulven T.

Int J Obes (Lond). 2016 Jul;40(7):1143-9. doi: 10.1038/ijo.2016.37. Epub 2016 Mar 16.


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

Hansen SV, 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.

J Med Chem. 2016 Mar 24;59(6):2841-6. doi: 10.1021/acs.jmedchem.5b01962. Epub 2016 Mar 15.


Distinct Phosphorylation Clusters Determine the Signaling Outcome of Free Fatty Acid Receptor 4/G Protein-Coupled Receptor 120.

Prihandoko R, Alvarez-Curto E, Hudson BD, Butcher AJ, Ulven T, Miller AM, Tobin AB, Milligan G.

Mol Pharmacol. 2016 May;89(5):505-20. doi: 10.1124/mol.115.101949. Epub 2016 Feb 12.


A protocol for amide bond formation with electron deficient amines and sterically hindered substrates.

Due-Hansen ME, Pandey SK, Christiansen E, Andersen R, Hansen SVF, Ulven T.

Org Biomol Chem. 2016 Jan 14;14(2):430-433. doi: 10.1039/c5ob02129d.


Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands.

Sergeev E, Hansen AH, Pandey SK, MacKenzie AE, Hudson BD, Ulven T, Milligan G.

J Biol Chem. 2016 Jan 1;291(1):303-17. doi: 10.1074/jbc.M115.687939. Epub 2015 Oct 29.


Dietary Fatty Acids and Their Potential for Controlling Metabolic Diseases Through Activation of FFA4/GPR120.

Ulven T, Christiansen E.

Annu Rev Nutr. 2015;35:239-63. doi: 10.1146/annurev-nutr-071714-034410. Review.


Comprehensive and quantitative profiling of lipid species in human milk, cow milk and a phospholipid-enriched milk formula by GC and MS/MSALL.

Sokol E, Ulven T, Færgeman NJ, Ejsing CS.

Eur J Lipid Sci Technol. 2015 Jun;117(6):751-759. Epub 2015 Feb 24.


Oxalyl chloride as a practical carbon monoxide source for carbonylation reactions.

Hansen SV, Ulven T.

Org Lett. 2015 Jun 5;17(11):2832-5. doi: 10.1021/acs.orglett.5b01252. Epub 2015 May 22.


Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases.

Christiansen E, Watterson KR, Stocker CJ, Sokol E, Jenkins L, Simon K, Grundmann M, Petersen RK, Wargent ET, Hudson BD, Kostenis E, Ejsing CS, Cawthorne MA, Milligan G, Ulven T.

Br J Nutr. 2015 Jun 14;113(11):1677-88. doi: 10.1017/S000711451500118X. Epub 2015 Apr 28.


Treatment of type 2 diabetes by free Fatty Acid receptor agonists.

Watterson KR, Hudson BD, Ulven T, Milligan G.

Front Endocrinol (Lausanne). 2014 Aug 28;5:137. doi: 10.3389/fendo.2014.00137. eCollection 2014. Review.


Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4.

Milligan G, Alvarez-Curto E, Watterson KR, Ulven T, Hudson BD.

Br J Pharmacol. 2015 Jul;172(13):3254-65. doi: 10.1111/bph.12879. Epub 2015 Feb 27. Review.


Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands.

Hudson BD, Christiansen E, Murdoch H, Jenkins L, Hansen AH, Madsen O, Ulven T, Milligan G.

Mol Pharmacol. 2014 Aug;86(2):200-10. doi: 10.1124/mol.114.093294. Epub 2014 May 28.


The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120).

Hudson BD, Shimpukade B, Milligan G, Ulven T.

J Biol Chem. 2014 Jul 18;289(29):20345-58. doi: 10.1074/jbc.M114.561449. Epub 2014 May 24.


Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4.

Butcher AJ, Hudson BD, Shimpukade B, Alvarez-Curto E, Prihandoko R, Ulven T, Milligan G, Tobin AB.

J Biol Chem. 2014 Jun 27;289(26):18451-65. doi: 10.1074/jbc.M114.568816. Epub 2014 May 9.


Direct N9-arylation of purines with aryl halides.

Larsen AF, Ulven T.

Chem Commun (Camb). 2014 May 21;50(39):4997-9. doi: 10.1039/c3cc48642g.


G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets.

Milligan G, Ulven T, Murdoch H, Hudson BD.

Br J Nutr. 2014 Jun;111 Suppl 1:S3-7. doi: 10.1017/S0007114513002249. Epub 2014 Jan 2.


Phenanthroline-2,9-bistriazoles as selective G-quadruplex ligands.

Nielsen MC, Larsen AF, Abdikadir FH, Ulven T.

Eur J Med Chem. 2014 Jan 24;72:119-26. doi: 10.1016/j.ejmech.2013.11.027. Epub 2013 Dec 5.


Structure-activity relationships and identification of optmized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators.

Chalikiopoulos A, Thiele S, Malmgaard-Clausen M, Rydberg P, Isberg V, Ulven T, Frimurer TM, Rosenkilde MM, Gloriam DE.

J Chem Inf Model. 2013 Nov 25;53(11):2863-73. doi: 10.1021/ci4003848. Epub 2013 Oct 22.


The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.

Hudson BD, Shimpukade B, Mackenzie AE, Butcher AJ, Pediani JD, Christiansen E, Heathcote H, Tobin AB, Ulven T, Milligan G.

Mol Pharmacol. 2013 Nov;84(5):710-25. doi: 10.1124/mol.113.087783. Epub 2013 Aug 26.


In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469.

Urban C, Hamacher A, Partke HJ, Roden M, Schinner S, Christiansen E, Due-Hansen ME, Ulven T, Gohlke H, Kassack MU.

Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30. doi: 10.1007/s00210-013-0899-3. Epub 2013 Jul 17.


Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5.

Rummel PC, Thiele S, Hansen LS, Petersen TP, Sparre-Ulrich AH, Ulven T, Rosenkilde MM.

Mol Pharmacol. 2013 Sep;84(3):335-45. doi: 10.1124/mol.113.086702. Epub 2013 Jun 13.


Multistep continuous-flow synthesis in medicinal chemistry: discovery and preliminary structure-activity relationships of CCR8 ligands.

Petersen TP, Mirsharghi S, Rummel PC, Thiele S, Rosenkilde MM, Ritzén A, Ulven T.

Chemistry. 2013 Jul 8;19(28):9343-50. doi: 10.1002/chem.201204350. Epub 2013 May 28.


Mucus can change the permeation rank order of drug candidates.

Hagesaether E, Christiansen E, Due-Hansen ME, Ulven T.

Int J Pharm. 2013 Aug 16;452(1-2):276-82. doi: 10.1016/j.ijpharm.2013.05.036. Epub 2013 May 23.


Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.

Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T.

ACS Med Chem Lett. 2013 May 9;4(5):441-445. Epub 2013 Apr 8.


Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor.

Hudson BD, Due-Hansen ME, Christiansen E, Hansen AM, Mackenzie AE, Murdoch H, Pandey SK, Ward RJ, Marquez R, Tikhonova IG, Ulven T, Milligan G.

J Biol Chem. 2013 Jun 14;288(24):17296-312. doi: 10.1074/jbc.M113.455337. Epub 2013 Apr 15.


Continuous flow nucleophilic aromatic substitution with dimethylamine generated in situ by decomposition of DMF.

Petersen TP, Larsen AF, Ritzén A, Ulven T.

J Org Chem. 2013 Apr 19;78(8):4190-5. doi: 10.1021/jo400390t. Epub 2013 Apr 2.


The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs.

Hudson BD, Ulven T, Milligan G.

Curr Top Med Chem. 2013;13(1):14-25. Review.


Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans.

Wagner R, Kaiser G, Gerst F, Christiansen E, Due-Hansen ME, Grundmann M, Machicao F, Peter A, Kostenis E, Ulven T, Fritsche A, Häring HU, Ullrich S.

Diabetes. 2013 Jun;62(6):2106-11. doi: 10.2337/db12-1249. Epub 2013 Feb 1.


Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability.

Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schmidt J, Hansen SV, Hudson BD, Zaibi M, Markussen SB, Hagesaether E, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T.

J Med Chem. 2013 Feb 14;56(3):982-92. doi: 10.1021/jm301470a. Epub 2013 Jan 22.


Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3.

Hudson BD, Tikhonova IG, Pandey SK, Ulven T, Milligan G.

J Biol Chem. 2012 Nov 30;287(49):41195-209. doi: 10.1074/jbc.M112.396259. Epub 2012 Oct 12.

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