Publications

2018

  • A. H. Hansen, E. Sergeev, D. Bolognini, R. R. Sprenger, J. H. Ekberg, C. S. Ejsing, C. J. McKenzie, Christine; E. Rexen Ulven, G. Milligan, T. Ulven. Discovery of a potent thiazolidine free fatty acid receptor 2 agonist with favorable pharmacokinetic properties. J. Med. Chem. 2018, 61, 9534-9550.
  • M. Schilperoort, A. D. van Dam, G. Hoeke, I. G. Shabalina, A. Okolo, A. C. Hanyaloglu, L. H. Dib, I. M. Mol, N. Caengprasath, Y.-W. Chan, S. Damak, A. R. Miller, T. Coskun, B. Shimpukade, T. Ulven, S. Kooijman, P. C. N. Rensen, M. Christian. The GPR120 agonist TUG-891 promotes metabolic 1 health by stimulating mitochondrial respiration in brown fat. EMBO Mol. Med. 2018, e8047.
  • S. F. Gallego, K. Højlund, C. S. Ejsing. Easy, Fast, and Reproducible Quantification of Cholesterol and Other Lipids in Human Plasma by Combined High Resolution MSX and FTMS Analysis. Am. Soc. Mass Spectrom. 2018, 1, 34-41.

2017

  • S. V. F. Hansen, T. Ulven. Pharmacological tool compounds for the free fatty acid receptor 4 (FFA4/GPR120). Handb. Exp. Pharmacol. 2017, 236, 33-56.
  • E. Sergeev, A. H. Hansen, D. Bolognini, K. Kawakami, T. Kishi, J. Aoki, T. Ulven, A. Inoue, B. Hudson, G. Milligan. A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias. Sci. Rep. 2017, 7, 13741.
  • A. H. Hansen, E. Sergeev, S. K. Pandey, B. D. Hudson, E. Christiansen, G. Milligan, T. Ulven. Development and characterization of a fluorescent tracer for the free fatty acid receptor 2 (FFA2/GPR43). J. Med. Chem. 2017, 60, 5638-5645.
  • M. H. Kaspersen, L. Jenkins, J. Dunlop, G. Milligan, T. Ulven. Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids at FFA1, FFA4 and GPR84. MedChemComm 2017, 8, 1360-1365.
  • N. R. V. Dragano, C. Solon, A. F. Ramalho, R. F. de Moura, D. S. Razolli, E. Christiansen, C. Azevedo, T. Ulven, L. A. Velloso. Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation. J. Neuroinflamm. 2017, 14, 91.
  • K. R. Watterson, S. V. F. Hansen, B. D. Hudson, E. Alvarez-Curto, S. Z. Raihan, C. M. G. Azevedo, G. Martin, J. Dunlop, S. J. Yarwood, T. Ulven, G. Milligan. Probe-dependent negative allosteric modulators of the long-chain free fatty acid receptor FFA4. Mol. Pharmacol. 2017, 91, 630-641.
  • J. M. Houthuijzen, I. Oosterom, B. D. Hudson, A. Hirasawa, L. G. M. Daenen, C. M. McLean, S. V. F. Hansen, M. T. M. van Jaarsveld, D. S. Peeper, S. Jafari Sadatmand, J. M. L. Roodhart, C. H. A. van de Lest, T. Ulven, K. Ishihara, G. Milligan, E. E.Voest. Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance. FASEB J. 2017, 31, 2195-2209.
  • G. Milligan, B. Shimpukade, T. Ulven, B. D. Hudson. Complex pharmacology of free fatty acid receptors. Chem. Rev. 2017, 117(1), 67-110. doi: 10.1021/acs.chemrev.6b00056.

2016

  • C. M. G. Azevedo, K. R. Watterson, E. T. Wargent, S. V. F. Hansen, B. D. Hudson, M. A. Kępczyńska, J. Dunlop, B. Shimpukade, E. Christiansen, G. Milligan, C. J. Stocker, T. Ulven. Non-acidic free fatty acid receptor 4 agonists with antidiabetic activity. J. Med. Chem. 2016, 59(19), 8868-8878.
  • L. Björkman, J. Mårtensson, M. Winther, M. Gabl, A. Holdfeldt, M. Uhrbom, J. Bylund, A. H. Hansen, S. Pandey, T. Ulven, H. Forsman, C. Dahlgren. The neutrophil response induced by an agonist for the free fatty acid receptor 2 (FFAR2/GPR43) is primed by the TNF-a and by receptor uncoupling from the cytoskeleton but attenuated by tissue recruitment. Mol. Cell Biol. 2016, 36(20), 2583-2595.
  • R. Prihandoko, E. Alvarez-Curto, B. D. Hudson, A. J. Butcher, T. Ulven, A. M. Miller, A. B. Tobin, G. Milligan. Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120. Mol. Pharmacol. 2016, 89(5), 505-520.
  • E. Christiansen, B. D. Hudson, A. H. Hansen, G. Milligan, T. Ulven. Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer. J. Med. Chem. 2016, 59(10), 4849-4858.
  • S. V. F. Hansen, E. Christiansen, C. Urban, B. D. Hudson, C. J. Stocker, M. E. Due-Hansen, E. T. Wargent, B. Shimpukade, R. Almeida, C. S. Ejsing, M. A. Cawthorne, M. U. Kassack, G. Milligan, T. Ulven. Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area and Robust in Vivo Efficacy. J. Med. Chem. 2016, 59(6), 2841-2846.
  • M. Grundmann, I. G. Tikhonova, B. D. Hudson, N. J. Smith, K. Mohr, T. Ulven, G. Milligan, T. Kenakin, E. Kostenis, A molecular mechanism for sequential activation of a G protein-coupled receptor. Cell Chem. Biol. 2016, 23, 392-403.
  • D. Gozal, Z. Qiao, I. Almendros, J. Zheng, A. Khalyfa, B. Shimpukade, T. Ulven. Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice. Int. J. Obese. 2016, 40(7), 1143-1149.
  • S. V. F. Hansen, Z. E. Wilson, T. Ulven, S. V. Ley. Controlled generation and use of CO in flow. React. Chem. Eng. 2016, 1, 280-287.
  • M. E. Due-Hansen, S. Pandey, E. Christiansen, R. Andersen, S. V. F. Hansen, T. Ulven. A protocol for amide bond formation with electron deficient amines and sterically hindered substrates. Org. Biomol. Chem. 2016, 14, 430-433.
  • E. Sergeev, A. H. Hansen, S. K. Pandey, A. E. Mackenzie, B. D. Hudson, T. Ulven, G. Milligan. Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. J. Biol. Chem. 2016, 291(1), 303-317.

2015

  • S. V. F. Hansen, T. Ulven. Oxalyl chloride as a practical carbon monoxide source for carbonylation reactions. Org. Lett. 2015, 17, 2832-2835. DOI: 10.1021/acs.orglett.5b01252.
  • T. Ulven, E. Christiansen. Dietary fatty acids and their potential for controlling metabolic diseases through activation of FFA4/GPR120. Annu. Rev. Nutr. 2015, 239-263.
  • E Christiansen, K. R. Watterson, C. J. Stocker, E. Sokol, L. Jenkins, K. Simon, M. Grundmann, R. K. Petersen, E. T. Wargent, B. D. Hudson, E. Kostenis, C. S. Ejsing, M. A. Cawthorne, G. Milligan, T. Ulven. Activity of dietary fatty acids on FFA1 and FFA4 and characterization of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases. Br. J. Nutr. 2015, 113, 1677-1688.
  • E. Sokol, T. Ulven, N. J. Færgeman, C. S. Ejsing. Comprehensive and quantitative profiling of lipid species in human milk, cow milk and a phospholipid-enriched milk formula by GC and MS/MSALL. Eur. J. Lipid Sci. Technol. 2015, 117, 751-759.
  • G. Milligan, E. Alvarez-Curto, K. R. Watterson, T. Ulven, B.D. Hudson. Characterising pharmacological ligands to study the long chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. Br. J. Pharmacol. 2015, 172(13), 3254-3265.

2014

  • B. D. Hudson, E. Christiansen, H. Murdoch, L. Jenkins, A. H. Hansen, O. Madsen, T. Ulven G. Milligan. Complex pharmacology of novel allosteric Free Fatty Acid 3 Receptor ligands. Mol. Pharmacol. 2014, 86, 200-210.
  • B. D. Hudson, B. Shimpukade, G. Milligan, T. Ulven. The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). J. Biol. Chem. 2014, 289, 20345-20358.
  • A. J. Butcher, B. D. Hudson, B. Shimpukade, E. Alvarez-Curto, R. Prihandoko, T. Ulven, G. Milligan, A. B. Tobin. Concomitant action of structural elements and receptor phosphorylation determine arrestin-3 interaction with the free fatty acid receptor FFA4. J. Biol. Chem. 2014, , 289, 18451-18465.
  • K. R. Watterson, B. D. Hudson, T. Ulven, G. Milligan. Treatment of type 2 diabetes by free fatty acid receptor agonists. Front. Endocrinol. 2014, 5, 137.
  • E. Fjaere, U. L. Aune, K. Roen, A. H. Keenan, T. Ma, K. Borokowsky, D. M. Kristensen, G. W. Novotny, T. Mandrup-Poulsen T, B. D. Hudson, G. Milligan, Y. Xi, J. W. Newman, F. G. Haj, B. Liaset, K. Kristiansen, L. Madsen. Indomethacin treatment prevents high-fat diet-induced obesity and insulin resistance, but not glucose intolerance in C57BL/6J mice. J Biol Chem. 2014 Apr 17.
  • G. Milligan, T. Ulven, H. Murdoch, B. D. Hudson. G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets. Br. J. Nutr. 2014, 111, S3-S7.

2013

  • B. D. Hudson, B. Shimpukade, A. E. Mackenzie, A. J. Butcher, J. D. Pediani, E. Christiansen, H. Heathcote, A. B. Tobin, T. Ulven, G. Milligan. The pharmacology of a potent and selective agonist, TUG-891, demonstrates both potential opportunity and possible challenges to therapeutic agonism of FFA4 (GPR120). Mol. Pharmacol. 2013, 84, 710-725.
  • B. D. Hudson, M. E. Due-Hansen, E. Christiansen, A. M. Hansen, A. E. Mackenzie, H. Murdoch, S. K. Pandey, R. J. Ward, R. Marquez, I. G. Tikhonova, T. Ulven, G. Milligan. Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. J. Biol. Chem. 2013, 288, 17296-17312.
  • E. Christiansen, S. V. F. Hansen, C. Urban, B. Hudson, E. T. Wargent, M. Grundmann, L. Jenkins, M. Zaibi, C. J. Stocker, S. Ullrich, E. Kostenis, M. U. Kassack, G. Milligan, M. A. Cawthorne, T. Ulven. Discovery of TUG-770: A highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. ACS Med. Chem. Lett. 2013, 4, 441–445.
  • E. Sokol, R. Almeida, H. K. Hannibal-Bach, D. Kotowska, J. Vogt, J. Baumgart, K. Kristiansen, R. Nitsch, J. Knudsen, C. S. Ejsing. Profiling of lipid species by normal-phase liquid chromatography, nanoelectrospray ionization, and ion trap–orbitrap mass spectrometry. Anal. Biochem. 2013, 443, 88–96.
  • B. D. Hudson, H. Murdoch, G. Milligan. Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids. Mol. Endocrinol. 2013, 27, 1177-1187.
  • B. D. Hudson, T. Ulven, G. Milligan. The Therapeutic Potential of Allosteric Ligands for Free Fatty Acid Sensitive GPCRs. Curr. Top. Med. Chem. 2013, 13, 14-25.
  • E. Christiansen, M. E. Due-Hansen, C. Urban, M. Grundmann, J. Schmidt, S. V. F. Hansen, B. D. Hudson, M. Zaibi, S. B. Markussen, E. Hagesaether, G. Milligan, M. A. Cawthorne, E. Kostenis, M. U. Kassack, T. Ulven. Discovery of a potent and selective FFA1 agonist with low lipophilicity and high oral bioavailability. Med. Chem. 2013, 56, 982-992.

2012

  • B. Shimpukade, B. D. Hudson, C. K. Hovgaard, G. Milligan, T. Ulven. Discovery of a potent and selective GPR120 agonist. J. Med. Chem. 2012, 55, 4511-4515.
  • E. Christiansen, M. E. Due-Hansen, C. Urban, M. Grundmann, R. Schröder, B. D. Hudson, G. Milligan, M. A. Cawthorne, E. Kostenis, M. U. Kassack, T. Ulven. Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J. Med. Chem. 2012, 55, 6243-6644.
  • B. D. Hudson, E. Christiansen, I. G. Tikhonova, M. Grundmann, E. Kostenis, D. R. Adams, T. Ulven, G. Milligan. Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. FASEB J. 2012, 26, 4951-4965.
  • T. Ulven. Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. Front. Endocrinol. 2012, 3, 111, doi:10.3389/fendo.2012.00111.
  • B. D. Hudson, I. G. Tikhonova, S. K. Pandey, T. Ulven, G. Milligan. Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. J. Biol. Chem. 2012, 287, 41195-41209.