Year |
Citation |
Score |
2024 |
Ieremias L, Kaspersen MH, Manandhar A, Schultz-Knudsen K, Vrettou CI, Pokhrel R, Heidtmann CV, Jenkins L, Kanellou C, Marsango S, Li Y, Bräuner-Osborne H, Rexen Ulven E, Milligan G, Ulven T. Structure-Activity Relationship Studies and Optimization of 4-Hydroxypyridones as GPR84 Agonists. Journal of Medicinal Chemistry. 67: 3542-3570. PMID 38381650 DOI: 10.1021/acs.jmedchem.3c01923 |
0.377 |
|
2023 |
Dragano NRV, Milbank E, Haddad-Tóvolli R, Garrido-Gil P, Nóvoa E, Fondevilla MF, Capelli V, Zanesco AM, Solon C, Morari J, Pires L, Estevez-Salguero Á, Beiroa D, González-García I, Barca-Mayo O, ... ... Ulven T, et al. Hypothalamic free fatty acid receptor-1 regulates whole-body energy balance. Molecular Metabolism. 101840. PMID 38036170 DOI: 10.1016/j.molmet.2023.101840 |
0.355 |
|
2023 |
Valentini A, Schultz-Knudsen K, Højgaard Hansen A, Tsakoumagkou A, Jenkins L, Christensen HB, Manandhar A, Milligan G, Ulven T, Rexen Ulven E. Discovery of Potent Tetrazole Free Fatty Acid Receptor 2 Antagonists. Journal of Medicinal Chemistry. 66: 6105-6121. PMID 37129317 DOI: 10.1021/acs.jmedchem.2c01935 |
0.402 |
|
2023 |
Kjær VMS, Daugvilaite V, Stepniewski TM, Madsen CM, Jørgensen AS, Bhuskute KR, Inoue A, Ulven T, Benned-Jensen T, Hjorth SA, Hjortø GM, Moo EV, Selent J, Rosenkilde MM. Migration mediated by the oxysterol receptor GPR183 depends on arrestin coupling but not receptor internalization. Science Signaling. 16: eabl4283. PMID 37014928 DOI: 10.1126/scisignal.abl4283 |
0.345 |
|
2022 |
Barki N, Bolognini D, Börjesson U, Jenkins L, Riddell J, Hughes DI, Ulven T, Hudson BD, Ulven ER, Dekker N, Tobin AB, Milligan G. Chemogenetics defines a short-chain fatty acid receptor gut-brain axis. Elife. 11. PMID 35229717 DOI: 10.7554/eLife.73777 |
0.342 |
|
2021 |
Hansen AH, Christensen HB, Pandey SK, Sergeev E, Valentini A, Dunlop J, Dedeo D, Fratta S, Hudson BD, Milligan G, Ulven T, Rexen Ulven E. Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2. Chemmedchem. PMID 34288488 DOI: 10.1002/cmdc.202100356 |
0.421 |
|
2021 |
Kjaer VMS, Ieremias L, Daugvilaite V, Lückmann M, Frimurer TM, Ulven T, Rosenkilde MM, Våbenø J. Discovery of GPR183 Agonists Based on an Antagonist Scaffold. Chemmedchem. PMID 34270165 DOI: 10.1002/cmdc.202100301 |
0.325 |
|
2021 |
Mårtensson J, Sundqvist M, Manandhar A, Leremias L, Zhang L, Ulven T, Xie X, Björkman L, Forsman H. The Two Formyl Peptide Receptors Differently Regulate GPR84-Mediated Neutrophil NADPH Oxidase Activity. Journal of Innate Immunity. 1-15. PMID 33789297 DOI: 10.1159/000514887 |
0.325 |
|
2020 |
Prihandoko R, Kaur D, Wiegman CH, Alvarez-Curto E, Donovan C, Chachi L, Ulven T, Tyas MR, Euston E, Dong Z, Alharbi AGM, Kim RY, Lowe JG, Hansbro PM, Chung KF, et al. Pathophysiological regulation of lung function by the free fatty acid receptor FFA4. Science Translational Medicine. 12. PMID 32817367 DOI: 10.1126/Scitranslmed.Aaw9009 |
0.401 |
|
2020 |
Engel DF, Bobbo VCD, Solon CS, Nogueira GA, Moura-Assis A, Mendes NF, Zanesco AM, Papangelis A, Ulven T, Velloso LA. Activation of GPR40 induces hypothalamic neurogenesis through p38- and BDNF-dependent mechanisms. Scientific Reports. 10: 11047. PMID 32632088 DOI: 10.1038/S41598-020-68110-2 |
0.349 |
|
2020 |
Rexen Ulven E, Quon T, Sergeev E, Barki N, Brvar M, Hudson BD, Dutta P, Hansen AH, Bielefeldt LØ, Tobin AB, McKenzie CJ, Milligan G, Ulven T. Structure-activity relationship studies of tetrahydroquinolone free fatty acid receptor 3 modulators. Journal of Medicinal Chemistry. PMID 32141297 DOI: 10.1021/Acs.Jmedchem.9B02036 |
0.477 |
|
2020 |
Sencio V, Barthelemy A, Tavares LP, Machado MG, Soulard D, Cuinat C, Queiroz-Junior CM, Noordine ML, Salomé-Desnoulez S, Deryuter L, Foligné B, Wahl C, Frisch B, Vieira AT, Paget C, ... ... Ulven T, et al. Gut Dysbiosis during Influenza Contributes to Pulmonary Pneumococcal Superinfection through Altered Short-Chain Fatty Acid Production. Cell Reports. 30: 2934-2947.e6. PMID 32130898 DOI: 10.1016/J.Celrep.2020.02.013 |
0.304 |
|
2019 |
Larsen O, Lückmann M, van der Velden WJC, Oliva-Santiago M, Brvar M, Ulven T, Frimurer TM, Karlshøj S, Rosenkilde MM. Selective Allosteric Modulation of N-Terminally Cleaved, but Not Full Length CCL3 in CCR1. Acs Pharmacology & Translational Science. 2: 429-441. PMID 32259075 DOI: 10.1021/acsptsci.9b00059 |
0.304 |
|
2019 |
Murtaza B, Hichami A, Khan AS, Shimpukade B, Ulven T, Ozdener MH, Khan NA. Novel GPR120 agonist TUG891 modulates fat taste perception and preference and activates tongue-brain-gut axis in mice. Journal of Lipid Research. PMID 31806728 DOI: 10.1194/Jlr.Ra119000142 |
0.377 |
|
2019 |
Köse M, Pillaiyar T, Namasivayam V, De Filippo E, Sylvester K, Ulven T, von Kügelgen I, Müller CE. An agonist radioligand for the proinflammatory lipid-activated G protein-coupled receptor GPR84 providing structural insights. Journal of Medicinal Chemistry. PMID 31721581 DOI: 10.1021/Acs.Jmedchem.9B01339 |
0.433 |
|
2018 |
Hansen AH, Sergeev E, Bolognini D, Sprenger RR, Ekberg JH, Ejsing CS, McKenzie CJ, Rexen Ulven E, Milligan G, Ulven T. Discovery of a Potent Thiazolidine Free Fatty Acid Receptor 2 Agonist with Favorable Pharmacokinetic Properties. Journal of Medicinal Chemistry. PMID 30247908 DOI: 10.1021/Acs.Jmedchem.8B00855 |
0.518 |
|
2018 |
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, et al. The GPR120 agonist TUG-891 promotes metabolic health by stimulating mitochondrial respiration in brown fat. Embo Molecular Medicine. PMID 29343498 DOI: 10.15252/Emmm.201708047 |
0.347 |
|
2018 |
Bourke J, Angeles R, Donovan C, Lam M, Micallef J, Shimpukade B, Ulven T, Royce S. Free fatty acid receptors, FFAR1 and FFAR4, are novel bronchodilator targets in mouse and human precision-cut lung slices European Respiratory Journal. 52. DOI: 10.1183/13993003.Congress-2018.Pa5259 |
0.386 |
|
2017 |
Kaspersen MH, Jenkins L, Dunlop J, Milligan G, Ulven T. Succinct synthesis of saturated hydroxy fatty acids and evaluation of all hydroxylauric acids on FFA1, FFA4 and GPR84. Medchemcomm. 8: 1360-1365. PMID 30108848 DOI: 10.1039/C7Md00130D |
0.43 |
|
2017 |
Mahmud ZA, Jenkins L, Ulven T, Labéguère F, Gosmini R, De Vos S, Hudson BD, Tikhonova IG, Milligan G. Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84. Scientific Reports. 7: 17953. PMID 29263400 DOI: 10.1038/S41598-017-18159-3 |
0.481 |
|
2017 |
Sergeev E, Hansen AH, Bolognini D, Kawakami K, Kishi T, Aoki J, Ulven T, Inoue A, Hudson BD, Milligan G. A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias. Scientific Reports. 7: 13741. PMID 29061999 DOI: 10.1038/S41598-017-14096-3 |
0.512 |
|
2017 |
Hansen AH, Sergeev E, Pandey SK, Hudson BD, Christiansen E, Milligan G, Ulven T. Development and characterization of a fluorescent tracer for the free fatty acid receptor 2 (FFA2/GPR43). Journal of Medicinal Chemistry. PMID 28570808 DOI: 10.1021/Acs.Jmedchem.7B00338 |
0.447 |
|
2017 |
Dragano NRV, Solon C, Ramalho AF, de Moura RF, Razolli DS, Christiansen E, Azevedo C, Ulven T, Velloso LA. Polyunsaturated fatty acid receptors, GPR40 and GPR120, are expressed in the hypothalamus and control energy homeostasis and inflammation. Journal of Neuroinflammation. 14: 91. PMID 28446241 DOI: 10.1186/S12974-017-0869-7 |
0.405 |
|
2017 |
Watterson KR, Hansen SV, Hudson B, Alvarez-Curto E, Raihan SZ, Azevedo CM, Martin G, Dunlop J, Yarwood SJ, Ulven T, Milligan G. Probe-dependent negative allosteric modulators of the long-chain free fatty acid receptor FFA4. Molecular Pharmacology. PMID 28385906 DOI: 10.1124/Mol.116.107821 |
0.541 |
|
2017 |
Houthuijzen JM, Oosterom I, Hudson BD, Hirasawa A, Daenen LG, McLean CM, Hansen SV, van Jaarsveld MT, Peeper DS, Jafari Sadatmand S, Roodhart JM, van de Lest CH, Ulven T, Ishihara K, Milligan G, et al. Fatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. PMID 28183801 DOI: 10.1096/Fj.201601248R |
0.347 |
|
2017 |
Hansen SV, Ulven T. Pharmacological Tool Compounds for the Free Fatty Acid Receptor 4 (FFA4/GPR120). Handbook of Experimental Pharmacology. 236: 33-56. PMID 27807695 DOI: 10.1007/164_2016_60 |
0.465 |
|
2016 |
Karlshøj S, Amarandi RM, Larsen O, Daugvilaite V, Steen A, Brvar M, Pui A, Frimurer TM, Ulven T, Rosenkilde MM. Molecular Mechanism of Action for Allosteric Modulators and Agonists in CC-chemokine Receptor 5 (CCR5). The Journal of Biological Chemistry. PMID 27834679 DOI: 10.1074/Jbc.M116.740183 |
0.388 |
|
2016 |
Azevedo CM, Watterson KR, Wargent ET, Hansen SV, Hudson BD, Kępczyńska MA, Dunlop J, Shimpukade B, Christiansen E, Milligan G, Stocker CJ, Ulven T. Non-Acidic Free Fatty Acid Receptor 4 Agonists with Antidiabetic Activity. Journal of Medicinal Chemistry. PMID 27570890 DOI: 10.1021/Acs.Jmedchem.6B00685 |
0.477 |
|
2016 |
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. THE NEUTROPHIL RESPONSE INDUCED BY AN AGONIST FOR THE FREE FATTY ACID RECEPTOR 2 (FFA2R/GPR43) IS PRIMED BY TNF-α AND BY RECEPTOR UNCOUPLING FROM THE CYTOSKELETON BUT ATTENUATED BY TISSUE RECRUITMENT. Molecular and Cellular Biology. PMID 27503855 DOI: 10.1128/Mcb.00161-16 |
0.478 |
|
2016 |
Milligan G, Shimpukade B, Ulven T, Hudson BD. Complex Pharmacology of Free Fatty Acid Receptors. Chemical Reviews. PMID 27299848 DOI: 10.1021/Acs.Chemrev.6B00056 |
0.495 |
|
2016 |
Christiansen E, Hudson BD, Hansen AH, Milligan G, Ulven T. Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer. Journal of Medicinal Chemistry. PMID 27074625 DOI: 10.1021/Acs.Jmedchem.6B00202 |
0.502 |
|
2016 |
Grundmann M, Tikhonova IG, Hudson BD, Smith NJ, Mohr K, Ulven T, Milligan G, Kenakin T, Kostenis E. A Molecular Mechanism for Sequential Activation of a G Protein-Coupled Receptor. Cell Chemical Biology. 23: 392-403. PMID 26991104 DOI: 10.1016/J.Chembiol.2016.02.014 |
0.479 |
|
2016 |
Gozal D, Qiao Z, Almendros I, Zheng J, Khalyfa A, Shimpukade B, Ulven T. Treatment with TUG891, a free fatty acid receptor 4 agonist, restores adipose tissue metabolic dysfunction following chronic sleep fragmentation in mice. International Journal of Obesity (2005). PMID 26980479 DOI: 10.1038/Ijo.2016.37 |
0.368 |
|
2016 |
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. 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. PMID 26928019 DOI: 10.1021/Acs.Jmedchem.5B01962 |
0.48 |
|
2016 |
Prihandoko R, Alvarez-Curto E, Hudson BD, Butcher AJ, Ulven T, Miller AM, Tobin AB, Milligan G. Distinct phosphorylation clusters determines the signalling outcome of the free fatty acid receptor FFA4/GPR120. Molecular Pharmacology. PMID 26873857 DOI: 10.1124/Mol.115.101949 |
0.4 |
|
2016 |
Houthuijzen J, Oosterom I, Hudson B, Hirasawa A, Daenen L, McLean C, Hansen S, Jaarsveld Mv, Peeper D, Sadatmand sJ, Roodhart J, Lest Cvd, Ulven T, Ishihara K, Milligan G, et al. Abstract 307: GPR120/FFAR4 activation by fatty acid 16:4(n-3) plays a key role in resistance to chemotherapy Cancer Research. 76: 307-307. DOI: 10.1158/1538-7445.Am2016-307 |
0.397 |
|
2015 |
Sergeev E, Hojgaard Hansen A, Pandey SK, Mackenzie AE, Hudson BD, Ulven T, Milligan G. Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands. The Journal of Biological Chemistry. PMID 26518871 DOI: 10.1074/Jbc.M115.687939 |
0.502 |
|
2015 |
Ulven T, Christiansen E. Dietary Fatty Acids and Their Potential for Controlling Metabolic Diseases Through Activation of FFA4/GPR120. Annual Review of Nutrition. 35: 239-63. PMID 26185978 DOI: 10.1146/Annurev-Nutr-071714-034410 |
0.413 |
|
2015 |
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. 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. The British Journal of Nutrition. 113: 1677-88. PMID 25916176 DOI: 10.1017/S000711451500118X |
0.464 |
|
2015 |
Milligan G, Alvarez-Curto E, Watterson KR, Ulven T, Hudson BD. Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4. British Journal of Pharmacology. 172: 3254-65. PMID 25131623 DOI: 10.1111/Bph.12879 |
0.518 |
|
2014 |
Watterson KR, Hudson BD, Ulven T, Milligan G. Treatment of type 2 diabetes by free Fatty Acid receptor agonists. Frontiers in Endocrinology. 5: 137. PMID 25221541 DOI: 10.3389/Fendo.2014.00137 |
0.496 |
|
2014 |
Hudson BD, Christiansen E, Murdoch H, Jenkins L, Hansen AH, Madsen O, Ulven T, Milligan G. Complex pharmacology of novel allosteric free fatty acid 3 receptor ligands. Molecular Pharmacology. 86: 200-10. PMID 24870406 DOI: 10.1124/Mol.114.093294 |
0.54 |
|
2014 |
Hudson BD, Shimpukade B, Milligan G, Ulven T. The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/GPR120). The Journal of Biological Chemistry. 289: 20345-58. PMID 24860101 DOI: 10.1074/Jbc.M114.561449 |
0.504 |
|
2014 |
Butcher AJ, Hudson BD, Shimpukade B, Alvarez-Curto E, Prihandoko R, Ulven T, Milligan G, Tobin AB. Concomitant action of structural elements and receptor phosphorylation determines arrestin-3 interaction with the free fatty acid receptor FFA4. The Journal of Biological Chemistry. 289: 18451-65. PMID 24817122 DOI: 10.1074/Jbc.M114.568816 |
0.474 |
|
2014 |
Milligan G, Ulven T, Murdoch H, Hudson BD. G-protein-coupled receptors for free fatty acids: nutritional and therapeutic targets. The British Journal of Nutrition. 111: S3-7. PMID 24382058 DOI: 10.1017/S0007114513002249 |
0.514 |
|
2014 |
Nielsen MC, Larsen AF, Abdikadir FH, Ulven T. Phenanthroline-2,9-bistriazoles as selective G-quadruplex ligands. European Journal of Medicinal Chemistry. 72: 119-26. PMID 24361524 DOI: 10.1016/J.Ejmech.2013.11.027 |
0.352 |
|
2013 |
Chalikiopoulos A, Thiele S, Malmgaard-Clausen M, Rydberg P, Isberg V, Ulven T, Frimurer TM, Rosenkilde MM, Gloriam DE. Structure-activity relationships and identification of optmized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators. Journal of Chemical Information and Modeling. 53: 2863-73. PMID 24083637 DOI: 10.1021/Ci4003848 |
0.444 |
|
2013 |
Hudson BD, Shimpukade B, Mackenzie AE, Butcher AJ, Pediani JD, Christiansen E, Heathcote H, Tobin AB, Ulven T, Milligan G. 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. Molecular Pharmacology. 84: 710-25. PMID 23979972 DOI: 10.1124/Mol.113.087783 |
0.505 |
|
2013 |
Urban C, Hamacher A, Partke HJ, Roden M, Schinner S, Christiansen E, Due-Hansen ME, Ulven T, Gohlke H, Kassack MU. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn-Schmiedeberg's Archives of Pharmacology. 386: 1021-30. PMID 23861168 DOI: 10.1007/S00210-013-0899-3 |
0.429 |
|
2013 |
Rummel PC, Thiele S, Hansen LS, Petersen TP, Sparre-Ulrich AH, Ulven T, Rosenkilde MM. Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5 Molecular Pharmacology. 84: 335-345. PMID 23765404 DOI: 10.1124/Mol.113.086702 |
0.459 |
|
2013 |
Petersen TP, Mirsharghi S, Rummel PC, Thiele S, Rosenkilde MM, Ritzén A, Ulven T. Multistep continuous-flow synthesis in medicinal chemistry: discovery and preliminary structure-activity relationships of CCR8 ligands. Chemistry (Weinheim An Der Bergstrasse, Germany). 19: 9343-50. PMID 23716302 DOI: 10.1002/Chem.201204350 |
0.412 |
|
2013 |
Hagesaether E, Christiansen E, Due-Hansen ME, Ulven T. Mucus can change the permeation rank order of drug candidates. International Journal of Pharmaceutics. 452: 276-82. PMID 23707884 DOI: 10.1016/J.Ijpharm.2013.05.036 |
0.324 |
|
2013 |
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. Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. Acs Medicinal Chemistry Letters. 4: 441-445. PMID 23687558 DOI: 10.1021/Ml4000673 |
0.447 |
|
2013 |
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. Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor. The Journal of Biological Chemistry. 288: 17296-312. PMID 23589301 DOI: 10.1074/Jbc.M113.455337 |
0.511 |
|
2013 |
Hudson BD, Ulven T, Milligan G. The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs. Current Topics in Medicinal Chemistry. 13: 14-25. PMID 23409763 DOI: 10.2174/1568026611313010004 |
0.449 |
|
2013 |
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. Reevaluation of fatty acid receptor 1 as a drug target for the stimulation of insulin secretion in humans. Diabetes. 62: 2106-11. PMID 23378609 DOI: 10.2337/Db12-1249 |
0.381 |
|
2013 |
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. Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. Journal of Medicinal Chemistry. 56: 982-92. PMID 23294321 DOI: 10.1021/Jm301470A |
0.485 |
|
2012 |
Hudson BD, Tikhonova IG, Pandey SK, Ulven T, Milligan G. Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. The Journal of Biological Chemistry. 287: 41195-209. PMID 23066016 DOI: 10.1074/Jbc.M112.396259 |
0.465 |
|
2012 |
Ulven T. Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. Frontiers in Endocrinology. 3: 111. PMID 23060857 DOI: 10.3389/Fendo.2012.00111 |
0.509 |
|
2012 |
Thiele S, Malmgaard-Clausen M, Engel-Andreasen J, Steen A, Rummel PC, Nielsen MC, Gloriam DE, Frimurer TM, Ulven T, Rosenkilde MM. Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors. Journal of Medicinal Chemistry. 55: 8164-77. PMID 22957890 DOI: 10.1021/Jm301121J |
0.445 |
|
2012 |
Hudson BD, Christiansen E, Tikhonova IG, Grundmann M, Kostenis E, Adams DR, Ulven T, Milligan G. Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 26: 4951-65. PMID 22919070 DOI: 10.1096/Fj.12-213314 |
0.469 |
|
2012 |
Larsen AF, Nielsen MC, Ulven T. Tetrasubstituted phenanthrolines as highly potent, water-soluble, and selective G-quadruplex ligands. Chemistry (Weinheim An Der Bergstrasse, Germany). 18: 10892-902. PMID 22807335 DOI: 10.1002/Chem.201200081 |
0.338 |
|
2012 |
Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schröder R, Hudson BD, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T. Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. Journal of Medicinal Chemistry. 55: 6624-8. PMID 22724451 DOI: 10.1021/Jm3002026 |
0.466 |
|
2012 |
Shimpukade B, Hudson BD, Hovgaard CK, Milligan G, Ulven T. Discovery of a potent and selective GPR120 agonist. Journal of Medicinal Chemistry. 55: 4511-5. PMID 22519963 DOI: 10.1021/Jm300215X |
0.489 |
|
2012 |
Schröder R, Xue L, Konya V, Martini L, Kampitsch N, Whistler JL, Ulven T, Heinemann A, Pettipher R, Kostenis E. PGH1, the precursor for the anti-inflammatory prostaglandins of the 1-series, is a potent activator of the pro-inflammatory receptor CRTH2/DP2. Plos One. 7: e33329. PMID 22442685 DOI: 10.1371/Journal.Pone.0033329 |
0.407 |
|
2012 |
Tyagi R, Shimpukade B, Blättermann S, Kostenis E, Ulven T. A concise synthesis of the potent inflammatory mediator 5-oxo-ETE Medchemcomm. 3: 195-198. DOI: 10.1039/C1Md00231G |
0.333 |
|
2011 |
Christiansen E, Urban C, Grundmann M, Due-Hansen ME, Hagesaether E, Schmidt J, Pardo L, Ullrich S, Kostenis E, Kassack M, Ulven T. Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. Journal of Medicinal Chemistry. 54: 6691-703. PMID 21854074 DOI: 10.1021/Jm2005699 |
0.511 |
|
2011 |
Larsen AF, Ulven T. Efficient synthesis of 4,7-diamino substituted 1,10-phenanthroline-2,9-dicarboxamides. Organic Letters. 13: 3546-8. PMID 21657265 DOI: 10.1021/Ol201321Z |
0.322 |
|
2011 |
Smith NJ, Ward RJ, Stoddart LA, Hudson BD, Kostenis E, Ulven T, Morris JC, Tränkle C, Tikhonova IG, Adams DR, Milligan G. Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Molecular Pharmacology. 80: 163-73. PMID 21498659 DOI: 10.1124/Mol.110.070789 |
0.52 |
|
2011 |
Schmidt J, Liebscher K, Merten N, Grundmann M, Mielenz M, Sauerwein H, Christiansen E, Due-Hansen ME, Ulven T, Ullrich S, Gomeza J, Drewke C, Kostenis E. Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40. The Journal of Biological Chemistry. 286: 11890-4. PMID 21339298 DOI: 10.1074/Jbc.C110.200477 |
0.378 |
|
2011 |
Schmidt J, Smith NJ, Christiansen E, Tikhonova IG, Grundmann M, Hudson BD, Ward RJ, Drewke C, Milligan G, Kostenis E, Ulven T. Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. The Journal of Biological Chemistry. 286: 10628-40. PMID 21220428 DOI: 10.1074/Jbc.M110.210872 |
0.51 |
|
2011 |
Tikhonova IG, Smith NJ, Ward RJ, Stoddart LA, Hudson BD, Kostenis E, Ulven T, Morris JC, Adams D, Milligan G. Probing Allosteric Binding Site Mapping in the Free Fatty Acid 2 receptor Biophysical Journal. 100: 52a. DOI: 10.1016/J.Bpj.2010.12.483 |
0.442 |
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2010 |
Christiansen E, Due-Hansen ME, Urban C, Merten N, Pfleiderer M, Karlsen KK, Rasmussen SS, Steensgaard M, Hamacher A, Schmidt J, Drewke C, Petersen RK, Kristiansen K, Ullrich S, Kostenis E, ... ... Ulven T, et al. Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. Acs Medicinal Chemistry Letters. 1: 345-9. PMID 24900217 DOI: 10.1021/Ml100106C |
0.473 |
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2010 |
Ulven T, Kostenis E. Novel CRTH2 antagonists: a review of patents from 2006 to 2009. Expert Opinion On Therapeutic Patents. 20: 1505-30. PMID 20946089 DOI: 10.1517/13543776.2010.525506 |
0.372 |
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2010 |
Christiansen E, Due-Hansen ME, Ulven T. A rapid and efficient Sonogashira protocol and improved synthesis of free fatty acid 1 (FFA1) receptor agonists. The Journal of Organic Chemistry. 75: 1301-4. PMID 20099863 DOI: 10.1021/Jo902533P |
0.436 |
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2010 |
Rist Ø, Grimstrup M, Receveur JM, Frimurer TM, Ulven T, Kostenis E, Högberg T. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorganic & Medicinal Chemistry Letters. 20: 1177-80. PMID 20031403 DOI: 10.1016/J.Bmcl.2009.12.008 |
0.487 |
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2010 |
Grimstrup M, Rist Ø, Receveur JM, Frimurer TM, Ulven T, Mathiesen JM, Kostenis E, Högberg T. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorganic & Medicinal Chemistry Letters. 20: 1181-5. PMID 20022749 DOI: 10.1016/J.Bmcl.2009.12.015 |
0.478 |
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2009 |
Nielsen MC, Borch J, Ulven T. Design, synthesis and evaluation of 4,7-diamino-1,10-phenanthroline G-quadruplex ligands. Bioorganic & Medicinal Chemistry. 17: 8241-6. PMID 19896385 DOI: 10.1016/J.Bmc.2009.09.055 |
0.311 |
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2009 |
Petersen TP, Ritzén A, Ulven T. A multistep continuous-flow system for rapid on-demand synthesis of receptor ligands. Organic Letters. 11: 5134-7. PMID 19852497 DOI: 10.1021/Ol902101C |
0.363 |
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2009 |
Schröder R, Merten N, Mathiesen JM, Martini L, Kruljac-Letunic A, Krop F, Blaukat A, Fang Y, Tran E, Ulven T, Drewke C, Whistler J, Pardo L, Gomeza J, Kostenis E. The C-terminal tail of CRTH2 is a key molecular determinant that constrains Galphai and downstream signaling cascade activation. The Journal of Biological Chemistry. 284: 1324-36. PMID 19010788 DOI: 10.1074/Jbc.M806867200 |
0.382 |
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2008 |
Christiansen E, Urban C, Merten N, Liebscher K, Karlsen KK, Hamacher A, Spinrath A, Bond AD, Drewke C, Ullrich S, Kassack MU, Kostenis E, Ulven T. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. Journal of Medicinal Chemistry. 51: 7061-4. PMID 18947221 DOI: 10.1021/Jm8010178 |
0.464 |
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2008 |
Jensen PC, Thiele S, Ulven T, Schwartz TW, Rosenkilde MM. Positive versus negative modulation of different endogenous chemokines for CC-chemokine receptor 1 by small molecule agonists through allosteric versus orthosteric binding. The Journal of Biological Chemistry. 283: 23121-8. PMID 18559339 DOI: 10.1074/Jbc.M803458200 |
0.389 |
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2007 |
Schratl P, Royer JF, Kostenis E, Ulven T, Sturm EM, Waldhoer M, Hoefler G, Schuligoi R, Lippe IT, Peskar BA, Heinemann A. The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking. Journal of Immunology (Baltimore, Md. : 1950). 179: 4792-9. PMID 17878378 DOI: 10.4049/Jimmunol.179.7.4792 |
0.389 |
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2007 |
Ulven T, Gallen MJ, Nielsen MC, Merten N, Schmidt C, Mohr K, Tränkle C, Kostenis E. Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2. Bioorganic & Medicinal Chemistry Letters. 17: 5924-7. PMID 17845848 DOI: 10.1016/J.Bmcl.2007.07.080 |
0.387 |
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2007 |
Royer JF, Schratl P, Lorenz S, Kostenis E, Ulven T, Schuligoi R, Peskar BA, Heinemann A. A novel antagonist of CRTH2 blocks eosinophil release from bone marrow, chemotaxis and respiratory burst. Allergy. 62: 1401-9. PMID 17714552 DOI: 10.1111/J.1398-9995.2007.01452.X |
0.371 |
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2007 |
Uller L, Mathiesen JM, Alenmyr L, Korsgren M, Ulven T, Högberg T, Andersson G, Persson CG, Kostenis E. Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respiratory Research. 8: 16. PMID 17328802 DOI: 10.1186/1465-9921-8-16 |
0.364 |
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2006 |
Ulven T, Receveur JM, Grimstrup M, Rist Ø, Frimurer TM, Gerlach LO, Mathiesen JM, Kostenis E, Uller L, Högberg T. Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. Journal of Medicinal Chemistry. 49: 6638-41. PMID 17154491 DOI: 10.1021/Jm060657G |
0.39 |
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2006 |
Ulven T, Kostenis E. Targeting the prostaglandin D2 receptors DP and CRTH2 for treatment of inflammation. Current Topics in Medicinal Chemistry. 6: 1427-44. PMID 16918458 DOI: 10.2174/15680266106061427 |
0.445 |
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2006 |
Kostenis E, Ulven T. Emerging roles of DP and CRTH2 in allergic inflammation. Trends in Molecular Medicine. 12: 148-58. PMID 16545607 DOI: 10.1016/J.Molmed.2006.02.005 |
0.397 |
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2006 |
Mathiesen JM, Christopoulos A, Ulven T, Royer JF, Campillo M, Heinemann A, Pardo L, Kostenis E. On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Molecular Pharmacology. 69: 1441-53. PMID 16418339 DOI: 10.1124/Mol.105.017681 |
0.477 |
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2006 |
Ulven T, Little PB, Receveur JM, Frimurer TM, Rist O, Nørregaard PK, Högberg T. 6-Acylamino-2-amino-4-methylquinolines as potent melanin-concentrating hormone 1 receptor antagonists: structure-activity exploration of eastern and western parts. Bioorganic & Medicinal Chemistry Letters. 16: 1070-5. PMID 16289819 DOI: 10.1016/J.Bmcl.2005.10.066 |
0.41 |
|
2006 |
Ulven T. Editorial [ Targeting G Protein-Coupled 7TM Receptors in Inflammation Guest Editor: Dr. Trond Ulven ] Current Topics in Medicinal Chemistry. 6: 1317-1318. DOI: 10.2174/15680266106061317 |
0.38 |
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2005 |
Ulven T, Frimurer TM, Receveur JM, Little PB, Rist O, Nørregaard PK, Högberg T. 6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. Journal of Medicinal Chemistry. 48: 5684-97. PMID 16134937 DOI: 10.1021/Jm050103Y |
0.414 |
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2005 |
Frimurer TM, Ulven T, Elling CE, Gerlach LO, Kostenis E, Högberg T. A physicogenetic method to assign ligand-binding relationships between 7TM receptors. Bioorganic & Medicinal Chemistry Letters. 15: 3707-12. PMID 15993056 DOI: 10.1016/J.Bmcl.2005.05.102 |
0.439 |
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2005 |
Mathiesen JM, Ulven T, Martini L, Gerlach LO, Heinemann A, Kostenis E. Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Molecular Pharmacology. 68: 393-402. PMID 15870392 DOI: 10.1124/Mol.104.010520 |
0.453 |
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2005 |
Ulven T, Kostenis E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. Journal of Medicinal Chemistry. 48: 897-900. PMID 15715457 DOI: 10.1021/Jm049036I |
0.438 |
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2004 |
Receveur JM, Bjurling E, Ulven T, Little PB, Nørregaard PK, Högberg T. 4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists. Bioorganic & Medicinal Chemistry Letters. 14: 5075-80. PMID 15380202 DOI: 10.1002/CHIN.200503102 |
0.412 |
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