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The global challenge of diabetes
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(b) Editorial. The global challenge of diabetes. Lancet 2008, 371, 1723.
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Editorial1
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Nolan, C. J.; Leahy, J. L.; Delghingaro-Augusto, V.; Moibi, J.; Soni, K.; Peyot, M. L.; Fortier, M.; Guay, C.; Lamontagne, J.; Barbeau, A.; Przybytkowski, E.; Joly, E.; Masiello, P.; Wang, S.; Mitchell, G. A.; Prentki, M. Beta cell compensation for insulin resistance in Zucker fatty rats: increased lipolysis and fatty acid signalling. Diabetologia 2006, 49, 2120-2130.
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1 for this receptor (http://www.iupdhar.org/). The receptor is also known as GPR40 and FFAR1.
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1 for this receptor (http://www.iupdhar.org/). The receptor is also known as GPR40 and FFAR1.
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5
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0037838892
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The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
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Briscoe, C. P.; Tadayyon, M.; Andrews, J. L.; Benson, W. G.; Chambers, J. K.; Eilert, M. M.; Ellis, C.; Elshourbagy, N. A.; Goetz, A. S.; Minnick, D. T.; Murdock, P. R.; Sauls, H. R., Jr.; Shabon, U.; Spinage, L. D.; Strum, J. C.; Szekeres, P. G.; Tan, K. B.; Way, J. M.; Ignar, D. M.; Wilson, S.; Muir, A. I. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J. Biol. Chem. 2003, 278, 11303-11311.
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6
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A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs
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Kotarsky, K.; Nilsson, N. E.; Flodgren, E.; Olde, B.; Owman, C. A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs. Biochem. Biophys. Res. Commun. 2003, 301, 406-410.
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7
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0037434991
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Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40
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Itoh, Y.; Kawamata, Y.; Harada, M.; Kobayashi, M.; Fujii, R.; Fukusumi, S.; Ogi, K.; Hosoya, M.; Tanaka, Y.; Uejima, H.; Tanaka, H.; Maruyama, M.; Satoh, R.; Okubo, S.; Kizawa, H.; Komatsu, H.; Matsumura, F.; Noguchi, Y.; Shinohara, T.; Hinuma, S.; Fujisawa, Y.; Fujino, M. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 2003, 422, 173-176.
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Itoh, Y.1
Kawamata, Y.2
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Hosoya, M.8
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Matsumura, F.17
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Hinuma, S.20
Fujisawa, Y.21
Fujino, M.22
more..
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8
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27944449329
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Free fatty acid receptor 1 (FFA(1)R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion
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Salehi, A.; Flodgren, E.; Nilsson, N. E.; Jimenez-Feltstrom, J.; Miyazaki, J.; Owman, C.; Olde, B. Free fatty acid receptor 1 (FFA(1)R/GPR40) and its involvement in fatty-acid-stimulated insulin secretion. Cell Tissue Res. 2005, 322, 207-215.
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Salehi, A.1
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Jimenez-Feltstrom, J.4
Miyazaki, J.5
Owman, C.6
Olde, B.7
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9
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25144433441
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Role of GPR40 in fatty acid action on the beta cell line INS-1E
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Shapiro, H.; Shachar, S.; Sekler, I.; Hershfinkel, M.; Walker, M. D. Role of GPR40 in fatty acid action on the beta cell line INS-1E. Biochem. Biophys. Res. Commun. 2005, 335, 97-104.
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Shapiro, H.1
Shachar, S.2
Sekler, I.3
Hershfinkel, M.4
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10
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33745607930
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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: Identification of agonist and antagonist small molecules
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Briscoe, C. P.; Peat, A. J.; McKeown, S. C.; Corbett, D. F.; Goetz, A. S.; Littleton, T. R.; McCoy, D. C.; Kenakin, T. P.; Andrews, J. L.; Ammala, C.; Fornwald, J. A.; Ignar, D. M.; Jenkinson, S. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br. J. Pharmacol. 2006, 148, 619-628.
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Briscoe, C.P.1
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McCoy, D.C.7
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Ammala, C.10
Fornwald, J.A.11
Ignar, D.M.12
Jenkinson, S.13
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11
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20944433543
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The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse
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Steneberg, P.; Rubins, N.; Bartoov-Shifman, R.; Walker, M. D.; Edlund, H. The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse. Cell Metab. 2005, 1, 245-258.
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Cell Metab
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Steneberg, P.1
Rubins, N.2
Bartoov-Shifman, R.3
Walker, M.D.4
Edlund, H.5
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12
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34047177401
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GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo
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Latour, M. G.; Alquier, T.; Oseid, E.; Tremblay, C.; Jetton, T. L.; Luo, J.; Lin, D. C.; Poitout, V. GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo. Diabetes 2007, 56, 1087-1094.
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Latour, M.G.1
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Luo, J.6
Lin, D.C.7
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13
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50949128408
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Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice
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Tan, C. P.; Feng, Y.; Zhou, Y. P.; Eiermann, G. J.; Petrov, A.; Zhou, C.; Lin, S.; Salituro, G.; Meinke, P.; Mosley, R.; Akiyama, T. E.; Einstein, M.; Kumar, S.; Berger, J. P.; Mills, S. G.; Thornberry, N. A.; Yang, L.; Howard, A. D. Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes 2008, 57, 2211-2219.
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Tan, C.P.1
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Einstein, M.12
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Berger, J.P.14
Mills, S.G.15
Thornberry, N.A.16
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Howard, A.D.18
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14
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52249093427
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The fatty-acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding
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Kebede, M.; Alquier, T.; Latour, M. G.; Semache, M.; Tremblay, C.; Poitout, V. The fatty-acid receptor GPR40 plays a role in insulin secretion in vivo after high-fat feeding. Diabetes 2008, 57, 2432-2437.
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Kebede, M.1
Alquier, T.2
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Semache, M.4
Tremblay, C.5
Poitout, V.6
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15
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51649104136
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Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization
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Vettor, R.; Granzotto, M.; De Stefani, D.; Trevellin, E.; Rossato, M.; Farina, M. G.; Milan, G.; Pilon, C.; Nigro, A.; Federspil, G.; Vigneri, R.; Vitiello, L.; Rizzuto, R.; Baratta, R.; Frittitta, L. Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization. J. Clin. Endocrinol. Metab. 2008, 93, 3541-3550.
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Federspil, G.10
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Vitiello, L.12
Rizzuto, R.13
Baratta, R.14
Frittitta, L.15
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16
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13844266013
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GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men
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Ogawa, T.; Hirose, H.; Miyashita, K.; Saito, I.; Saruta, T. GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men. Metabolism 2005, 54, 296-299.
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Ogawa, T.1
Hirose, H.2
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Saruta, T.5
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17
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19944434042
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Studies of relationships between variation of the human G protein-coupled receptor 40 gene and type 2 diabetes and insulin release
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Hamid, Y. H.; Vissing, H.; Holst, B.; Urhammer, S. A.; Pyke, C.; Hansen, S. K.; Glumer, C.; Borch-Johnsen, K.; Jorgensen, T.; Schwartz, T. W.; Pedersen, O.; Hansen, T. Studies of relationships between variation of the human G protein-coupled receptor 40 gene and type 2 diabetes and insulin release. Diabetic Med. 2005, 22, 74-80.
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Hamid, Y.H.1
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Glumer, C.7
Borch-Johnsen, K.8
Jorgensen, T.9
Schwartz, T.W.10
Pedersen, O.11
Hansen, T.12
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18
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53849146735
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The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: Investigations using GPR40-knockout mice
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Discussion on agonsts vs antagonists as FFA1 modulators for type 2 diabetes
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1 modulators for type 2 diabetes: Brownlie, R.; Mayers, R. M.; Pierce, J. A.; Marley, A. E.; Smith, D. M. The long-chain fatty acid receptor, GPR40, and glucolipotoxicity: investigations using GPR40-knockout mice. Biochem. Soc. Trans. 2008, 36, 950-954.
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Brownlie, R.1
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Marley, A.E.4
Smith, D.M.5
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19
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33144463383
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Synthesis and activity of small molecule GPR40 agonists
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Garrido, D. M.; Corbett, D. F.; Dwornik, K. A.; Goetz, A. S.; Littleton, T. R.; McKeown, S. C.; Mills, W. Y.; Smalley, T. L., Jr.; Briscoe, C. P.; Peat, A. J. Synthesis and activity of small molecule GPR40 agonists. Bioorg. Med. Chem. Lett. 2006, 16, 1840-1845.
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Garrido, D.M.1
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McKeown, S.C.6
Mills, W.Y.7
Smalley Jr., T.L.8
Briscoe, C.P.9
Peat, A.J.10
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20
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33847104280
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Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor
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McKeown, S. C.; Corbett, D. F.; Goetz, A. S.; Littleton, T. R.; Bigham, E.; Briscoe, C. P.; Peat, A. J.; Watson, S. P.; Hickey, D. M. Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor. Bioorg. Med. Chem. Lett. 2007, 17, 1584-1589.
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McKeown, S.C.1
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Peat, A.J.7
Watson, S.P.8
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21
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34250879091
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Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists
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Song, F.; Lu, S.; Gunnet, J.; Xu, J. Z.; Wines, P.; Proost, J.; Liang, Y.; Baumann, C.; Lenhard, J.; Murray, W. V.; Demarest, K. T.; Kuo, G. H. Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists. J. Med. Chem. 2007, 50, 2807-2817.
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Song, F.1
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Liang, Y.7
Baumann, C.8
Lenhard, J.9
Murray, W.V.10
Demarest, K.T.11
Kuo, G.H.12
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22
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39149097541
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Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening
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Tikhonova, I. G.; Sum, C. S.; Neumann, S.; Engel, S.; Raaka, B. M.; Costanzi, S.; Gershengorn, M. C. Discovery of novel agonists and antagonists of the free fatty acid receptor 1 (FFAR1) using virtual screening. J. Med. Chem. 2008, 51, 625-633.
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Tikhonova, I.G.1
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Neumann, S.3
Engel, S.4
Raaka, B.M.5
Costanzi, S.6
Gershengorn, M.C.7
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23
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0035991325
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Functional screening of G protein-coupled receptors by measuring intracellular calcium with a fluorescence microplate reader
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Kassack, M. U.; Hofgen, B.; Lehmann, J.; Eckstein, N.; Quillan, J. M.; Sadee, W. Functional screening of G protein-coupled receptors by measuring intracellular calcium with a fluorescence microplate reader. J. Biomol. Screening 2002, 7, 233-246.
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Kassack, M.U.1
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Eckstein, N.4
Quillan, J.M.5
Sadee, W.6
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24
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56749167283
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50 of 6.35 ± 0.03 and an efficacy of 123% relative to linoleic acid.
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50 of 6.35 ± 0.03 and an efficacy of 123% relative to linoleic acid.
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25
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56749135676
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50 and log P (calculated by ChemBioDraw, version 11.0) for compounds 11-16 and 19 was 0.98
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50 and log P (calculated by ChemBioDraw, version 11.0) for compounds 11-16 and 19 was 0.98.
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26
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40749084402
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Evaluation of dynamic mass redistribution technology for pharmacological studies of recombinant and endogenously expressed G protein-coupled receptors
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Lee, P. H.; Gao, A.; van Staden, C.; Ly, J.; Salon, J.; Xu, A.; Fang, Y.; Verkleeren, R. Evaluation of dynamic mass redistribution technology for pharmacological studies of recombinant and endogenously expressed G protein-coupled receptors. Assay Drug Dev. Technol. 2008, 6, 83-94.
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Lee, P.H.1
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Ly, J.4
Salon, J.5
Xu, A.6
Fang, Y.7
Verkleeren, R.8
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27
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45149110002
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Label-free cell-based assays for GPCR screening
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Fang, Y.; Frutos, A. G.; Verklereen, R. Label-free cell-based assays for GPCR screening. Comb. Chem. High Throughput Screening 2008, 11, 357-369.
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Fang, Y.1
Frutos, A.G.2
Verklereen, R.3
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28
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20144389835
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Serum- and glucocorticoid-inducible kinase 1 (SGK1) mediates glucocorticoid-induced inhibition of insulin secretion
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Ullrich, S.; Berchtold, S.; Ranta, F.; Seebohm, G.; Henke, G.; Lupescu, A.; Mack, A. F.; Chao, C. M.; Su, J.; Nitschke, R.; Alexander, D.; Friedrich, B.; Wulff, P.; Kuhl, D.; Lang, F. Serum- and glucocorticoid-inducible kinase 1 (SGK1) mediates glucocorticoid-induced inhibition of insulin secretion. Diabetes 2005, 54, 1090-1099.
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Mack, A.F.7
Chao, C.M.8
Su, J.9
Nitschke, R.10
Alexander, D.11
Friedrich, B.12
Wulff, P.13
Kuhl, D.14
Lang, F.15
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29
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34347220548
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Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition
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Tikhonova, I. G.; Sum, C. S.; Neumann, S.; Thomas, C. J.; Raaka, B. M.; Costanzi, S.; Gershengorn, M. C. Bidirectional, iterative approach to the structural delineation of the functional "chemoprint" in GPR40 for agonist recognition. J. Med. Chem. 2007, 50, 2981-2989.
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Tikhonova, I.G.1
Sum, C.S.2
Neumann, S.3
Thomas, C.J.4
Raaka, B.M.5
Costanzi, S.6
Gershengorn, M.C.7
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