Publications

2024

• Structure-Activity Relationship Studies and Optimization of 4-Hydroxypyridones as GPR84 Agonists. Ieremias, M. H. Kaspersen, A. Manandhar, K. Schultz-Knudsen, C. I. Vrettou, R. Pokhrel, C. V. Heidtmann, L. Jenkins, C. Kanellou, S. Marsango, Y. Li, H. Bräuner-Osborne, E. Rexen Ulven, G. Milligan, T. Ulven. J. Med. Chem. 2024, 79, 3542-3570.
• Chronic administration of hydrolysed pine nut oil to mice improves insulin sensitivity and glucose tolerance and increases energy expenditure via a free fatty acid receptor 4-dependent mechanism. E.T. Wargent, M.A Kępczyńska, M.H. Kaspersen, E.R Ulven, J.R.S. Arch, T. Ulven, C.J. Stocker. Br. J. Nutr. 2024, May 16:1-8.
• Drug Repurposing in Crohn’s Disease Using Danish Real-World Data. Shakibfar, K. H. Allin, T. Jess, M. A. Barbieri, V. Battini, E. Simoncic, J. Kirchgesner, T. Ulven, M. Sessa. Pragmat. Obs. Res. 2024, 15, 17-29.
• Hypothalamic free fatty acid receptor-1 regulates whole-body energy balance.R.V. Dragano, E. Milbank, R. Haddad-Tóvolli, P. Garrido-Gil, E. Nóvoa, M.F. Fondevilla, V. Capelli, A.M. Zanesco, C. Solon, J. Morari, L. Pires, Á. Estevez-Salguero, D. Beiroa, I. González-García, O. Barca-Mayo, C. Diéguez, R. Nogueiras, J.L. Labandeira-García, E.R. Ulven, T. Ulven, M. Claret, LA. Velloso, M. Lopez. Mol Metab. 2024, 79, 101840.

2023

• Functional Group-Tolerant Pd-catalyzed Carbonylative Negishi Coupling with Aryl Iodides. Kalinin, T. Ulven. J. Org. Chem. 2023, 88(23), 16633-16638.
• Identification of 5-HT2 serotonin receptor modulators through the synthesis of a diverse, tropane- and quinuclidine-alkaloid-inspired compound library. R. Yao, A. Jensen, H. Bryce-Rogers, K. Schultz-Knudsen, L. Zhou, N. Hovendal, H. Pedersen, M. Kubus, T. Ulven, L. Laraia. J. Med. Chem. 2023, 66(16), 11536-11554.

• Development and Characterization of Potent Succinate Receptor Fluorescent Tracers. M. Ciba, D. Dibnah , B.D. Hudson, E. Rexen Ulven. J. Med. 2023, 66(13), 8951-8974.
• Glucose-stimulated insulin secretion depends on FFA1 and Gq in neonatal mouse islets. Lorza-Gil, G. Kaiser, C. Carlein, M.D.A. Hoffmann, G.M. König, S. Haug, L. Prates Roma, E. Rexen Ulven, T. Ulven, E. Kostenis, A.L. Birkenfeld, H.U. Häring, S. Ullrich, F. Gerst. Diabetologia 2023, 66(8), 1501-1515.

• Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists. A. Valentini, K. Schultz-Knudsen, A. Højgaard Hansen, A. Tsakoumagkou, L. Jenkins, H.B. Christensen, A. Manandhar, G. Milligan, T. Ulven, E. Rexen Ulven. J. Med. Chem. 2023, 66(9), 6105-6121.
• Migration mediated by the oxysterol receptor GPR183 depends on arrestin coupling but not receptor internalization. V.M.S. Kjær, V. Daugvilaite, T.M. Stepniewski, C.M. Madsen, A.S. Jørgensen, K.R. Bhuskute, A. Inoue, T. Ulven, T. Benned-Jensen, S.A. Hjorth, G.M. Hjortø, E.V. Moo, J. Selent, M.M. Rosenkilde. Sci. Signal. 2023, 16(779), eabl4283.
• Structure-activity relationship of GPR15L peptide analogues and investigation of their interaction with the GPR15 receptor. Y. Deng, C.V. Perez Almeria, L. van Gijzel, K. Schaller, L. Vedel, D.E. Gloriam, T. Ulven, H. Bräuner-Osborne. Basic Clin. Pharmacol. Toxicol. 2023, 132(6), 459-471.
• Ligand entry pathways control the chemical space recognized by GPR183. V.M.S. Kjær, T.M. Stępniewski, B. Medel-Lacruz, L. Reinmuth, M. Ciba, E. Rexen Ulven, M. Bonomi, J. Selent, M.M. Rosenkilde. Chem Sci. 2023, 14(39), 10671-10683.
• Identification of galectin-1 and other cellular targets of alpha,beta-unsaturated carbonyl compounds, including dimethylfumarate, by use of click-chemistry probes. B. Sauerland, C. Helm, L. G. Lorentzen, A. Manandhar, T. Ulven, L. F. Gamon, M. J. Davies. Redox Biol. 2023, 59, 102560.

2022

• Synthesis of lysophosphatidylcholine and mixed phosphatidylcholine. A. Papangelis, T. Ulven. J. Org. Chem. 2022, 87(12), 8194-8197.
• Synthesis and cellular evaluation of click-chemistry probes to study the biological effects of alpha, beta-unsaturated carbonyls. C. Morozzia, M. Sauerland, L.F. Gamon, A. Manandhar, T. Ulven, M.J. Davies. Redox Biol. 2022, (8 pages).
• Chemogenetics defines a short chain fatty acid receptor gut-brain axis. N. Barki, D. Bolognini, U. Börjesson, L. Jenkins, J. Riddell, D. I. Hughes, T. Ulven, B. D. Hudson, E. Rexen Ulven, N. Dekker, A. B. Tobin, G. Milligan. eLife 2022, 11:e73777 (23 pages).

2021

• Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. A. H. Hansen, H. B. Christensen, S. K. Pandey, E. Sergeev, A. Valentini, J. Dunlop, D. Dedeo, S. Fratta, B. D. Hudson, G. Milligan, T. Ulven, E. Rexen Ulven. ChemMedChem 2021, 16(21), 3326-3341.
• Acute effects of delayed-release hydrolyzed pine nut oil on glucose tolerance, incretins, ghrelin and appetite in healthy humans. K. V. Sørensen, S. S. Korfitzen, M. H. Kaspersen, E. Rexen Ulven, J. H. Ekberg, A. Bauer-Brandl, T. Ulven, K. Højlund. Clin. Nutr. 2021, 40, 2169-2179.
• Discovery of GPR183 Agonists Based on an Antagonist Scaffold. V. M. S. Kjær, L. Ieremias, V. Daugvilaite, M. Lückmann, T. M. Frimurer, T. Ulven, M. Rosenkilde, J. Våbenø. ChemMedChem 2021, 16(17), 2623-2627.
• One-Pot Synthesis of Xanthone by Carbonylative Suzuki Coupling Reaction. D. R. P. Loureiro, J. X. Soares, A. Maia, A. M. N. Silva, M. Rangel, C. M. G. Azevedo, S. Hansen, T. Ulven, M. M. M. Pinto, S. Reis, C. M. M. Afonso. ChemistrySelect 2021, 6, 4511-4514.
• The Two Formyl Peptide Receptors Differently Regulate GPR84-Mediated Neutrophil NADPH Oxidase Activity. J. Mårtensson, M. Sundqvist, A. Manandhar, L. Ieremias, L. Zhang, T. Ulven, X. Xie, L. Björkman, H. Forsman. J Innate Immun 2021, 13(4), 242-256.

2020

• Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators. E. Rexen Ulven, T. Quon, E. Sergeev, N. Barki, M. Brvar, B. D. Hudson, P. Dutta, A. H. Hansen, L. Ø. Bielefeldt, A. B. Tobin, C. J. McKenzie, G. Milligan, T. Ulven. J. Med. Chem. 2020, 63, 3577-3595.
• An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights. M. Köse, T. Pillaiyar, V. Namasivayam, E. De Filippo, K. Sylvester, T. Ulven, I. Von Kügelgen, C. E. Müller.  J. Med. Chem. 2020, 63, 2391-2410.
• Gut Dysbiosis during Influenza Contributes to Pulmonary Pneumococcal Superinfection through Altered Short-Chain Fatty Acid Production. V. Sencio, A. Barthelemy, L. P. Tavares, M. G. Machado, D. Soulard, C. Cuinat, C. M. Queiroz-Junior, M. L. Noordine, S. Salomé-Desnoulez, L. Deryuter, B. Foligné, C. Wahl, B. Frisch, A. T. Vieira, C. Paget, G. Milligan, T. Ulven, I. Wolowczuk, C. Faveeuw, R. Le Goffic, M. Thomas, S. Ferreira, M. M. Teixeira, F. Trottein. Cell Rep. 2020, 30, 2934-2947.
• Activation of GPR40 induces hypothalamic neurogenesis through p38-and BDNF-dependent mechanisms. D. F. Engel, V. C. D. Bobbo, C. S. Solon, G. A. Nogueira, A. Moura-Assis, N. F. Mendes, A. M. Zanesco, A. Papangelis, T. Ulven, L. A. Velloso. Sci. Rep. 2020, 10, 11047.
• Autocrine negative feed-back regulation of lipolysis through sensing of NEFAs by FFAR4/GPR120 in WAT. A. S. Husted, J. H. Ekberg, E. Tripp, T. A. D. Nissen, S. Meijnikman, S. L. O’Brien, T. Ulven, Y. Acherman, S. C. Bruin, M. Nieuwdorp, Z. Gerhart-Hines, D. Calebiro, L. O. Dragsted, T. W. Schwartz. Mol Metab. 2020, 42, 101103.
• FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells. E. Lorza-Gil, G. Kaiser, E. Rexen Ulven, G. M. Koenig, F. Gerst, M. B. Oquendo, A. L. Birkenfeld, H. Haering, E. Kostenis, T. Ulven, S. Ullrich. Sci. Rep. 2020, 10, 16497.
• Novel GPR120 agonist TUG891 modulates fat taste perception and preference and activates tongue-brain-gut axis in mice. B. Murtaza, A. Hichami, A. S. Khan, B. Shimpukade, T. Ulven, M. H. Ozdener, N. A. Khan. J. Lipid Res. 2020, 61, 133-142.
• Pathophysiological regulation of lung function by the free fatty acid receptor FFA4. R. Prihandoko, D. Kaur, C. H. Wiegman, E. Alvarez-Curto, C. Donovan, L. Chachi, T. Ulven, M. R. Tyas, E. Euston, Z. Dong, A. G. M. Alharbi, R. Y. Kim, J. G. Lowe, P. M. Hansbro, K. F. Chung, C. E. Brightling, G. Milligan, A. B. Tobin. Sci. Transl. Med. 2020, 12, 9009.

2019

• Butyrate ameliorates allergic airway inflammation by limiting eosinophil trafficking and survival. A. Theiler, T. Bärnthaler, W. Platzer, G. Richtig, M. Peinhaupt, S. Rittchen, J. Kargl, T. Ulven, L. M. Marsh, G. Marsche, R. Schuligoi, E. M. Sturm, A. Heinemann. J. Allergy Clin. Immunol. 2019, 144, 764-776.
• Selective Allosteric Modulation of N-Terminally Cleaved, but Not Full Length CCL3 in CCR1. O. Larsen, M. Lückmann, W. J. C. van der Velden, M. Oliva-Santiago, M. Brvar, T. Ulven, T. M. Frimurer, S. Karlshøj, M. Rosenkilde. ACS Pharmacol. Transl. Sci. 2019, 2, 429-441.
• Kan fedtsyrer bruges som medicin? E. Rexen Ulven. Aktuel Naturvidenskab 2019, 3, 19-22.

2018

• Discovery of a potent thiazolidine free fatty acid receptor 2 agonist with favorable pharmacokinetic properties. 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. J. Med. Chem. 2018, 61, 9534-9550. [READ PAPER]
• Dihydropyridine fluorophores allow for specific detection of human antibodies in serum. I. Domljanovic, E. Rexen Ulven, T. Ulven, R. P. Thomsen, A. H. Okholm, J. Kjems, A. Voss, M. Taskova, K. Astakhova. ACS Omega 2018, 3, 7580-7586. [READ PAPER]
• Structure-Activity Investigations and Optimisations of Non-metabolite Agonists for the Succinate Receptor 1. E. Rexen Ulven, M. Trauelsen, M. Brvar, M. Lückmann, L. Ø. Bielefeldt, L. K. I Jensen, T. W. Schwartz, T. M. Frimurer. Sci. Rep. 2018, 8, 10010. [READ PAPER]
• The GPR120 agonist TUG-891 promotes metabolic 1 health by stimulating mitochondrial respiration in brown fat. 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. EMBO Mol. Med. 2018, e8047. [READ PAPER]

2017

• Receptor structure-based discovery of non-metabolite agonists for the succinate receptor GPR91. M. Trauelsen, E. Rexen Ulven, S.A. Hjorth, M. Brvar, C. Monaco, T.M. Frimurer, T.W. Schwartz. Mol. Metab. 2017, 6, 1585-1596.
• Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84. Al Mahmud, L. Jenkins, T. Ulven, F. Labéguère, R. Gosmini, S. De Vos, B. D. Hudson, I. G. Tikhonova, Graeme Milligan. Sci. Rep. 2017, 7, 17953.
• A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias. Sergeev, A. H. Hansen, D. Bolognini, K. Kawakami, T. Kishi, J. Aoki, T. Ulven, A. Inoue, B. Hudson, G. Milligan.  Sci. Rep. 2017, 7, 13741.

• Development and characterization of a fluorescent tracer for the free fatty acid receptor 2 (FFA2/GPR43). A. H. Hansen, E. Sergeev, S. K. Pandey, B. D. Hudson, E. Christiansen, G. Milligan, T. Ulven. J. Med. Chem. 2017, 60, 5638-5645. 

• Succinct synthesis of saturated hydroxy fatty acids and in vitro evaluation of all hydroxylauric acids at FFA1, FFA4 and GPR84. M. H. Kaspersen, L. Jenkins, J. Dunlop, G. Milligan, T. Ulven. MedChemComm 2017, 8, 1360-1365.
• Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation. 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. J. Neuroinflamm. 2017, 14, 91.
• Probe-dependent negative allosteric modulators of the long-chain free fatty acid receptor FFA4. 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. Mol. Pharmacol. 2017, 91, 630-641.
• Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance. 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. FASEB J. 2017, 31, 2195-2209.

• Complex pharmacology of free fatty acid receptors. G. Milligan, B. Shimpukade, T. Ulven, B. D. Hudson. Chem. Rev. 2017, 117(1), 67-110.
• Pharmacological tool compounds for the free fatty acid receptor 4 (FFA4/GPR120). S. V. F. Hansen, T. Ulven. Handb. Exp. Pharmacol. 2017, 236, 33-56.

2016

• Molecular mechanism of action for allosteric modulators and agonists in CC-chemokine receptor 5 (CCR5). S. Karlshøj, R. M. Amarandi, O. Larsen, V. Daugvilaite, A. Steen, M. Brvar, A. Pui, T. M. Frimurer, T. Ulven, M. M. Rosenkilde. J. Biol. Chem. 2016, 291(52), 26860-26874.

• Non-acidic free fatty acid receptor 4 agonists with antidiabetic activity. 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. J. Med. Chem. 2016, 59(19), 8868-8878.
• 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. 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. Mol. Cell Biol. 2016, 36(20), 2583-2595.

• Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer. E. Christiansen, B. D. Hudson, A. H. Hansen, G. Milligan, T. Ulven. J. Med. Chem. 2016, 59(10), 4849-4858.

• Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice. D. Gozal, Z. Qiao, I. Almendros, J. Zheng, A. Khalyfa, B. Shimpukade, T. Ulven. Int. J. Obese. 2016, 40(7), 1143-1149.

• Discovery of a potent free fatty acid 1 receptor agonist with low lipophilicity, low polar surface area and robust in vivo efficacy. 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. J. Med. Chem. 2016, 59(6), 2841-2846.
• A molecular mechanism for sequential activation of a G protein-coupled receptor. M. Grundmann, I. G. Tikhonova, B. D. Hudson, N. J. Smith, K. Mohr, T. Ulven, G. Milligan, T. Kenakin, E. Kostenis. Cell Chem. Biol. 2016, 23, 392-403.

• Controlled generation and use of CO in flow. S. V. F. Hansen, Z. E. Wilson, T. Ulven, S. V. Ley. React. Chem. Eng. 2016, 1, 280-287. 
• Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120. R. Prihandoko, E. Alvarez-Curto, B. D. Hudson, A. J. Butcher, T. Ulven, A. M. Miller, A. B. Tobin, G. Milligan. Mol. Pharmacol. 2016, 89(5), 505-520. 

• A protocol for amide bond formation with electron deficient amines and sterically hindered substrates. M. E. Due-Hansen, S. Pandey, E. Christiansen, R. Andersen, S. V. F. Hansen, T. Ulven. Org. Biomol. Chem. 2016, 14, 430-433.
• Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. E. Sergeev, A. H. Hansen, S. K. Pandey, A. E. Mackenzie, B. D. Hudson, T. Ulven, G. Milligan. J. Biol. Chem. 2016, 291(1), 303-317.

2015

• Oxalyl chloride as a practical carbon monoxide source for carbonylation reactions. S. V. F. Hansen, T. Ulven. Org. Lett. 2015, 17, 2832-2835.
• Dietary fatty acids and their potential for controlling metabolic diseases through activation of FFA4/GPR120. T. Ulven, E. Christiansen. Annu. Rev. Nutr. 2015, 239-263.
• 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. 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. Br. J. Nutr. 2015, 113, 1677-1688.
• Comprehensive and quantitative profiling of lipid species in human milk, cow milk and a phospholipid-enriched milk formula by GC and MS/MS^ALL. E. Sokol, T. Ulven, N. J. Færgeman, C. S. Ejsing. Eur. J. Lipid Sci. Technol. 2015, 117, 751-759.
• Characterising pharmacological ligands to study the long chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. G. Milligan, E. Alvarez-Curto, K. R. Watterson, T. Ulven, B.D. Hudson. Br. J. Pharmacol. 2015, 172(13), 3254-3265.

2014

• Treatment of type 2 diabetes by free fatty acid receptor agonists. K. R. Watterson, B. D. Hudson, T. Ulven, G. Milligan. Front. Endocrinol. 2014, 5, 137.
• Complex pharmacology of novel allosteric Free Fatty Acid 3 Receptor ligands. B. D. Hudson, E. Christiansen, H. Murdoch, L. Jenkins, A. H. Hansen, O. Madsen, T. Ulven, G. Milligan. Mol. Pharmacol. 2014, 86, 200-210.

• The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). B. D. Hudson, B. Shimpukade, G. Milligan, T. Ulven. J. Biol. Chem. 2014, 289, 20345-20358.
• Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4. A. J. Butcher, B. D. Hudson, B. Shimpukade, E. Alvarez-Curto, R. Prihandoko, T. Ulven, G. Milligan, A. B. Tobin. J. Biol. Chem. 2014, 289, 18451-18465.

• Direct N⁹-coupling of purines with aryl halides. A. F. Larsen, T. Ulven. Chem. Commun. 2014, 50, 4997-4999.
• G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets. G. Milligan, T. Ulven, H. Murdoch, B. D. Hudson. Br. J. Nutr. 2014, 111, S3-S7.

• Phenanthroline-2,9-bistriazoles as selective G-quadruplex ligands. M. C. Nielsen, A. F. Larsen, F. H. Abdikadir, T. Ulven. Eur. J. Med. Chem. 2014, 72, 119-126.

2013

• Discovery of TUG-770: A highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist for treatment of type 2 diabetes. 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. ACS Med. Chem. Lett. 2013, 4, 441–445.
• Structure-activity relationships and identification of optimized CC-chemokine receptor CCR1, 5 and 8 metal-ion chelators. A. Chalikiopoulos, S. Thiele, M. Malmgaard-Clausen, P. Rydberg, V. Isberg, T. Ulven, T. M. Frimurer, M. M. Rosenkilde, D. E. Gloriam. J. Chem. Inf. Model. 2013, 53(11), 2863-2873.
• The pharmacology of a potent and selective agonist, TUG-891, demonstrates both potential opportunity and possible challenges to therapeutic agonism of FFA4 (GPR120). 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. Mol. Pharmacol. 2013, 84, 710-725.
• In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. C. Urban, A. Hamacher, H. J. Partke, M. Roden, S. Schinner, E. Christiansen, M. E. Due-Hansen, T. Ulven, H. Gohlke, M. U. Kassack. Naunyn Schmiedebergs Arch. Pharmacol. 2013, 386(12), 1021-30.
• Extracellular Disulfide Bridges Serve Different Purposes in Two Homologous Chemokine Receptors, CCR1 and CCR5. P. C. Rummel, S. Thiele, L. S. Hansen, T. P. Petersen, A. H. Sparre-Ulrich, T. Ulven, M. M. Rosenkilde. Mol. Pharmacol. 2013, 84, 335-345.

• Mucus can change the permeation rank order of drug candidates. E. Hagesaether, E. Christiansen, M. E. Due-Hansen, T. Ulven. Int. J. Pharm. 2013, 452, 276-282.
• Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. 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. J. Biol. Chem. 2013, 288, 17296-17312.

• Continuous flow nucleophilic aromatic substitution with dimethylamine generated in situ by decomposition of DMF. T. P. Petersen, A. F. Larsen, A. Ritzén, T. Ulven. J. Org. Chem. 2013, 78, 4190–4195.

• Multistep Continuous Flow Synthesis in Medicinal Chemistry: Discovery and Preliminary Structure-Activity Relationships of CCR8 Ligands. T. P. Petersen, S. Mirsharghi, P. C. Rummel, S. Thiele, M. M. Rosenkilde, A. Ritzén, T. Ulven. Chem. Eur. J. 2013, 19, 9343-9350.
• Reevaluation of FFAR1 as drug target for the treatment of insulin deficiency in humans. R. Wagner, G. Kaiser, F. Gerst, E. Christiansen, M. Due-Hansen, M. Grundmann, F. Machicao, A. Peter, E. Kostenis, T. Ulven, A. Fritsche, H.-U. Häring, S. Ullrich. Diabetes 2013, 62, 2106-2111.

• Discovery of a potent and selective FFA1 agonist with low lipophilicity and high oral bioavailability. 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. J. Med. Chem. 2013, 56(3), 982-992.
• The Therapeutic Potential of Allosteric Ligands for Free Fatty Acid Sensitive GPCRs. B. D. Hudson, T. Ulven, G. Milligan. Curr. Top. Med. Chem. 2013, 13, 14-25.

• Selective copper catalysed aromatic N-arylation in water. J. Engel-Andreasen, B. Shimpukade, T. Ulven. Green Chem. 2013, 15, 336-340.

2012

• Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. B. D. Hudson, I. G. Tikhonova, S. K. Pandey, T. Ulven, G. Milligan. J. Biol. Chem. 2012, 287, 41195-41209.

• Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. T. Ulven. Front. Endocrinol. 2012, 3, 111.

• Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. S. Thiele, M. Malmgaard-Clausen, J. Engel-Andreasen, A. Steen, P. C. Rummel, M. C. Nielsen, D. E. Gloriam, T. M. Frimurer, T. Ulven, M. M. Rosenkilde. J. Med. Chem. 2012, 55(18), 8164-8177.
• Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. B. D. Hudson, E. Christiansen, I. G. Tikhonova, M. Grundmann, E. Kostenis, D. R. Adams, T. Ulven, G. Milligan. FASEB J. 2012, 26, 4951-4965.

• Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties. 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. J. Med. Chem. 2012, 55(14), 6624-6628.

• Tetrasubstituted phenanthrolines as highly potent, water soluble and selective G‑quadruplex ligands. A. F. Larsen, M. C. Nielsen, T. Ulven. Chem. Eur. J. 2012, 18(35), 10892-10902.

• Discovery of a potent and selective GPR120 agonist. B. Shimpukade, B. D. Hudson, C. K. Hovgaard, G. Milligan, T. Ulven. J. Med. Chem. 2012, 55(9), 4511-4515.

• A biased ligand for OXE-R uncouples Ga and Gbg signaling within a heterotrimer. S. Blättermann, L. Peters, P. A. Ottersbach, A. Bock, V. Konya, C. D. Weaver, A. Gonzalez, R. Schröder, R. Tyagi, P. Luschnig, J. Gäb, S. Hennen, T. Ulven, L. Pardo, K. Mohr, M. Gütschow, A. Heinemann, E. Kostenis. Nature Chem. Biol. 2012, 8(7), 631-638.
• PGH1, the precursor for the anti-inflammatory prostaglandins of the 1-series, is a potent activator of the pro-inflammatory receptor CRTH2/DP2. R. Schröder, L. Xue, V. Konya, L. Martini, N. Kampitsch, J. L. Whistler, T. Ulven, A. Heinemann, R. Pettipher, E. Kostenis. PLoS One 2012, 7, e33329.

• A concise synthesis of the potent inflammatory mediator 5-oxo-ETE. R. Tyagi, B. Shimpukade, S. Blättermann, E. Kostenis, T. Ulven. MedChemComm 2012, 3, 195-198.

• The oxygen-mediated synthesis of 1,3-butadiynes in continuous flow: Using Teflon AF-2400 to effect gas/liquid contact. T. P. Petersen, A. Polyzos, M. O´Brien, T. Ulven, I. R. Baxendale, S. V. Ley. ChemSusChem 2012, 5, 274-277.

2011

• Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. E. Christiansen, C. Urban, M. Grundmann, M. Due-Hansen, E. Hagesaether, J. Schmidt, L. Pardo, S. Ullrich, E. Kostenis, M. Kassack, T. Ulven. J. Med. Chem. 2011, 54, 6691-6703.

• Efficient synthesis of 4,7-diamino substituted 1,10-phenanthroline-2,9-dicarboxamides. A. F. Larsen, T. Ulven. Org. Lett. 2011, 13(13), 3546-3548.
• Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. N. J. Smith, R. J. Ward, L. A. Stoddart, B. D. Hudson, E. Kostenis, T. Ulven, J. C. Morris, C. Trankle, I. G. Tikhonova, D. R. Adams, G. Milligan. Mol. Pharmacol. 2011, 80(1), 163-173.
• Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40. J. Schmidt, K. Liebscher, N. Merten, M. Grundmann, M. Mielenz, H. Sauerwein, E. Christiansen, M. E. Due-Hansen, T. Ulven, S. Ullrich, J. Gomeza, C. Drewke, E. Kostenis. J. Biol. Chem. 2011, 286(14), 11890-11894.
• Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. J. Schmidt, N. J. Smith, E. Christiansen, I. G. Tikhonova, M. Grundmann, B. D. Hudson, R. J. Ward, C. Drewke, G. Milligan, E. Kostenis, T. Ulven. J. Biol. Chem. 2011, 286(12), 10628-10640.

2010

• Structure-activity study of para-substituted dihydro­cinnamic acids: Discovery of the potent and selective FFA1 (GPR40) receptor agonist TUG-469. E. Christiansen, M. E. Due-Hansen, C. Urban, N. Merten, M. Pfleiderer, K. K. Karlsen, S. S. Rasmussen, M. Steensgaard, A. Hamacher, J. Schmidt, C. Drewke, R. K. Petersen, K. Kristiansen, S. Ullrich, E. Kostenis, M. U. Kassack, T. Ulven. ACS Med. Chem. Lett. 2010, 1(7), 345-349.
• Novel CRTH2 antagonists: a review of patents from 2006 to 2009. T. Ulven, E. Kostenis. Expert Opin. Ther. Pat. 2010, 20(11), 1505-1530.
• Macrocyclic G-quadruplex ligands. M. C. Nielsen, T. Ulven. Curr. Med. Chem. 2010, 17(29), 3438-3448.

• A rapid and efficient Sonogashira protocol and improved synthesis of free fatty acid 1 (FFA1) receptor agonists. E. Christiansen, M. E. Due-Hansen, T. Ulven. J. Org. Chem. 2010, 75(4), 1301-1304.
• Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. M. Grimstrup, Ø. Rist, J.-M. Receveur, T. M. Frimurer, T. Ulven, J. M. Mathiesen, E. Kostenis, T. Högberg. Bioorg. Med. Chem. Lett. 2010, 20(3), 1181-1185.
• Novel selective thiazoleacetic acids as CRTfH2 antagonists developed from in silico derived hits. Part 1. Ø. Rist, M. Grimstrup, J.-M. Receveur, T. M. Frimurer, T. Ulven, E. Kostenis, T. Högberg. Bioorg. Med. Chem. Lett. 2010, 20(3), 1177-1180.

2009

• A multistep continuous flow system for rapid on-demand synthesis of receptor ligands. T. P. Petersen, A. Ritzén, T. Ulven. Org. Lett. 2009, 11(22), 5134-5137.
• Design, synthesis and evaluation of 4,7-diamino-1,10-phenanthroline G-quadruplex ligands. M. C. Nielsen, J. Borch, T. Ulven. Bioorg. Med. Chem. 2009, 17(24), 8242-8246.
• The C-terminal tail of CRTH2 is a key molecular determinant that constrains Gai- and downstream-signaling cascade activation. R. Schroeder, N. Merten, J. M. Mathiesen, L. Martini, A. K. Letunic, F. Krop, A. Blaukat, Y. Fang, E. Tran, T. Ulven, C. Drewke, J. Whistler, L. Pardo, J. Gomeza, E. Kostenis. J. Biol. Chem. 2009, 284(2), 1324-1336.
• 4-Fluoro-N-methyl-N-(1,2,3,4-tetrahydrocarbazol-3-yl)benzenesulfonamide. K. G. Rasmussen, T. Ulven, A. D. Bond. Acta Cryst. 2009, E65, o742.
• Ethyl 2-(1,2,3,4-tetrahydrospiro[carbazole-3,2′-[1,3]dioxolan]-9-yl)acetate. P. M. G. Löffler, T. Ulven, A. D. Bond. Acta Cryst. 2009, E65, o685.
• 1,2-Dihydrospiro[carbazole-3(4H),2′-[1,3]dioxolane]. J. V. Bjerrum, T. Ulven, A. D. Bond. Acta Cryst. 2009, E65, o579.

2008

• Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA1/GPR40), a potential target for the treatment of type II diabetes. E. Christiansen, C. Urban, N. Merten, K. Liebscher, K. K. Karlsen, A. Hamacher, A. Spinrath, A. D. Bond, C. Drewke, S. Ullrich, M. U. Kassack, E. Kostenis, T. Ulven. J. Med. Chem. 2008, 51(22), 7061-7064.
• Selective extraction of G-quadruplex ligands from a rationally designed scaffold-based dynamic combinatorial library. M. C. Nielsen, T. Ulven. Chem. Eur. J. 2008, 14(31), 9487-9490.
• Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric binding. P. C. Jensen, S. Thiele, T. Ulven, T. W. Schwartz, M. M. Rosenkilde. J. Biol. Chem. 2008, 283(34), 23121-23128.

2007

• Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D₂ receptor CRTH2. T. Ulven, M. J. Gallen, M. C. Nielsen, N. Merten, C. Schmidt, K. Mohr, C. Tränkle, E. Kostenis. Bioorg. Med. Chem. Lett. 2007, 17(21), 5924-2927.
• The role of the prostaglandin D₂ receptor, DP, in eosinophil trafficking. P. Schratl, J. F. Royer, E. Kostenis, T. Ulven, E. M. Sturm, M. Waldhoer, G. Hoefler, R. Schuligoi, I. T. Lippe, B. A. Peskar, A Heinemann. J. Immunol. 2007, 179(7), 4792-4799.
• A novel antagonist of CRTH2 blocks eosinophil release from bone marrow, chemotaxis and respiratory burst. J. F. Royer, P. Schratl, S. Lorenz, E. Kostenis, T. Ulven, R. Schuligoi, B. A. Peskar, A. Heinemann. Allergy 2007, 62(12), 1401-1409.
• Antagonism of the prostaglandin D₂ receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. L. Uller, J. M. Mathiesen, L. Alenmyr, M. Korsgren, T. Ulven, T. Högberg, G. Andersson, C. G. A. Persson, E. Kostenis. Respir. Res. 2007, 8, 16.

2006

• Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. T. Ulven, J.-M. Receveur, M. Grimstrup, Ø. Rist, T. M. Frimurer, L.-O. Gerlach, J. M. Mathiesen, E. Kostenis, L. Uller, T. Högberg. J. Med. Chem. 2006, 49(23), 6638-6641.
• Targeting the prostaglandin D₂ receptors DP and CRTH2 for treatment of inflammation. T. Ulven, E. Kostenis. Curr. Top. Med. Chem. 2006, 6(13), 1427-1444.
• Emerging roles of DP and CRTH2 in allergic inflammation. E. Kostenis, T. Ulven. Trends Mol. Med. 2006, 12(4), 148-158.
• On the mechanism of interaction of potent, surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. J. M. Mathiesen, A. Christopoulos, T. Ulven, J. Royer, M. Campillo, A. Heinemann, L. Pardo, E. Kostenis. Mol. Pharmacol. 2006, 69(4), 1441-1453.
• 6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists – Structure-activity exploration of eastern and western parts. T. Ulven, P. B. Little, J.-M. Receveur, T. M. Frimurer, Ø. Rist, P. K. Nørregaard, T. Högberg. Bioorg. Med. Chem. Lett. 2006, 16(4), 1070-1075.

2005

• 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists – Identification, SAR and investigation of binding mode. T. Ulven, T. M. Frimurer, J.-M. Receveur, P. B. Little, Ø. Rist, P. K. Nørregaard, T. Högberg. J. Med. Chem. 2005, 48(18), 5684-5697.
• A physicogenetic method to assign ligand-binding relationships between 7TM receptors. T. M. Frimurer, T. Ulven, C. E. Ellingf, L.-O. Gerlach, E. Kostenis, T. Högberg. Bioorg. Med. Chem. Lett. 2005, 15(16), 3707-3712.
• Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. J. M. Mathiesen, T. Ulven, L. Martini, L.-O. Gerlach, A. Heinemann, E. Kostenis. Mol. Pharmacol. 2005, 68(2), 393-402.
• Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. T. Ulven, E. Kostenis. J. Med. Chem. 2005, 48(4), 897-900.