-
1
-
-
0031581088
-
A cluster of four novel human G proteincoupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1
-
Sawzdargo, M.; George, S.R.; Nguyen, T.; Xu, S.; Kolakowski, L.F.; O'Dowd, B.F. A cluster of four novel human G proteincoupled receptor genes occurring in close proximity to CD22 gene on chromosome 19q13.1. Biochem. Biophys. Res. Commun., 1997, 239(2), 543-547.
-
(1997)
Biochem. Biophys. Res. Commun
, vol.239
, Issue.2
, pp. 543-547
-
-
Sawzdargo, M.1
George, S.R.2
Nguyen, T.3
Xu, S.4
Kolakowski, L.F.5
O'Dowd, B.F.6
-
2
-
-
58149095589
-
International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1,-2, and-3: Pharmacology and pathophysiological functions
-
Stoddart, L.A.; Smith, N.J.; Milligan, G. International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1,-2, and-3: pharmacology and pathophysiological functions. Pharmacol. Rev., 2008, 60(4), 405-417.
-
(2008)
Pharmacol. Rev
, vol.60
, Issue.4
, pp. 405-417
-
-
Stoddart, L.A.1
Smith, N.J.2
Milligan, G.3
-
3
-
-
0037838892
-
The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
-
Briscoe, C.P.; Tadayyon, M.; Andrews, J.L.; Benson, W.G.; Chambers, J.K.; Eilert, M.M.; Ellis, C.E.; Elshourbagy, N.A.; Goetz, A.S.; Minnick, D.T.; Murdock, P.R.; Sauls, H.R. Jr.; Shabon, U.; Spinage, L.D.; Strum, J.C.; Szekers, 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(13), 11303-11311.
-
(2003)
J. Biol. Chem
, vol.278
, Issue.13
, pp. 11303-11311
-
-
Briscoe, C.P.1
Tadayyon, M.2
Andrews, J.L.3
Benson, W.G.4
Chambers, J.K.5
Eilert, M.M.6
Ellis, C.E.7
Elshourbagy, N.A.8
Goetz, A.S.9
Minnick, D.T.10
Murdock, P.R.11
Sauls Jr., H.R.12
Shabon, U.13
Spinage, L.D.14
Strum, J.C.15
Szekers, P.G.16
Tan, K.B.17
Way, J.M.18
Ignar, D.M.19
Wilson, S.20
Muir, A.I.21
more..
-
4
-
-
0037434991
-
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
-
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 β cells through GPR40. Nature, 2003, 422(6928), 173-176.
-
(2003)
Nature
, vol.422
, Issue.6928
, pp. 173-176
-
-
Itoh, Y.1
Kawamata, Y.2
Harada, M.3
Kobayashi, M.4
Fujii, R.5
Fukusumi, S.6
Ogi, K.7
Hosoya, M.8
Tanaka, Y.9
Uejima, H.10
Tanaka, H.11
Maruyama, M.12
Satoh, R.13
Okubo, S.14
Kizawa, H.15
Komatsu, H.16
Matsumura, F.17
Noguchi, Y.18
Shinohara, T.19
Hinuma, S.20
Fujisawa, Y.21
Fujino, M.22
more..
-
5
-
-
0038363378
-
The Orphan G Protein-coupled Receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids
-
Brown, A.J.; Goldsworthy, S.M.; Barnes, A.A.; Eilert, M.M.; Tcheang, L.; Daniels, D.; Muir, A.I.; Wigglesworth, M.J.; Kinghorn, I.; Fraser, N.J.; Pike, N.B.; Strum, J.C.; Steplewski, K.M.; Murdock, P.R.; Holder, J.C.; Marshall, F.H.; Szekeres, P.G.; Wilson, S.; Ignar, D.M.; Foord, S.M.; Wise, A.; Dowell, S.J. The Orphan G Protein-coupled Receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids. J. Biol. Chem. 2003, 278(13), 11312-11319.
-
(2003)
J. Biol. Chem
, vol.278
, Issue.13
, pp. 11312-11319
-
-
Brown, A.J.1
Goldsworthy, S.M.2
Barnes, A.A.3
Eilert, M.M.4
Tcheang, L.5
Daniels, D.6
Muir, A.I.7
Wigglesworth, M.J.8
Kinghorn, I.9
Fraser, N.J.10
Pike, N.B.11
Strum, J.C.12
Steplewski, K.M.13
Murdock, P.R.14
Holder, J.C.15
Marshall, F.H.16
Szekeres, P.G.17
Wilson, S.18
Ignar, D.M.19
Foord, S.M.20
Wise, A.21
Dowell, S.J.22
more..
-
6
-
-
0038491435
-
Functional characterization of human receptors for Short Chain fatty acids and their role in polymorphonuclear cell activation
-
Le Poul, E.; Loison, C.; Struyf, S.; Springael, J.Y.; Lannoy, V.; Decobecq, M.E.; Brezillon, S.; Dupriez, V.; Vassart, G.; Van Damme, J.; Parmentier, M.; Detheux, M. Functional characterization of human receptors for Short Chain fatty acids and their role in polymorphonuclear cell activation. J. Biol. Chem. 2003, 278(28), 25481-25489.
-
(2003)
J. Biol. Chem
, vol.278
, Issue.28
, pp. 25481-25489
-
-
Le Poul, E.1
Loison, C.2
Struyf, S.3
Springael, J.Y.4
Lannoy, V.5
Decobecq, M.E.6
Brezillon, S.7
Dupriez, V.8
Vassart, G.9
van Damme, J.10
Parmentier, M.11
Detheux, M.12
-
7
-
-
0037453280
-
Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids
-
Nilsson, NE.; Kotarsky, K.; Owman, C.; Olde, B. Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids. Biochem. Biophys. Res. Commun. 2003, 303(4), 1047-1052.
-
(2003)
Biochem. Biophys. Res. Commun
, vol.303
, Issue.4
, pp. 1047-1052
-
-
Nilsson, N.E.1
Kotarsky, K.2
Owman, C.3
Olde, B.4
-
8
-
-
13444263540
-
Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
-
Hirasawa, A.; Tsumaya, K.; Awaji, T.; Katsuma, S.; Adachi, T.; Tamada, M.; Sugimoto, Y.; Miyazaki, S.; Tsujimoto, G. Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120. Nat. Med., 2005, 11(1), 90-94.
-
(2005)
Nat. Med
, vol.11
, Issue.1
, pp. 90-94
-
-
Hirasawa, A.1
Tsumaya, K.2
Awaji, T.3
Katsuma, S.4
Adachi, T.5
Tamada, M.6
Sugimoto, Y.7
Miyazaki, S.8
Tsujimoto, G.9
-
9
-
-
77956165390
-
GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects
-
Oh, D.Y.; Talukdar, S.; Bae, E.J.; Imamura, T.; Morinaga, H.; Fan, W.; Li, P.; Lu, W.J.; Watkins, S.M.; Olefsky, J.M. GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects. Cell. 2010, 142(5), 687-698.
-
(2010)
Cell
, vol.142
, Issue.5
, pp. 687-698
-
-
Oh, D.Y.1
Talukdar, S.2
Bae, E.J.3
Imamura, T.4
Morinaga, H.5
Fan, W.6
Li, P.7
Lu, W.J.8
Watkins, S.M.9
Olefsky, J.M.10
-
10
-
-
33845954973
-
Mediumchain fatty acids as ligands for orphan G protein-coupled receptor GPR84
-
Wang, J.; Wu, X.; Simonavicius, N.; Tian, H.; Ling, L. Mediumchain fatty acids as ligands for orphan G protein-coupled receptor GPR84. J. Biol. Chem., 2006, 281(45), 34457-34464.
-
(2006)
J. Biol. Chem
, vol.281
, Issue.45
, pp. 34457-34464
-
-
Wang, J.1
Wu, X.2
Simonavicius, N.3
Tian, H.4
Ling, L.5
-
11
-
-
47749128507
-
Seven transmembrane spanning receptors for free fatty acids as therapeutic targets for diabetes mellitus: Pharmacological, phylogenetic and drug discovery aspects
-
Costanzi, S.; Neumann, S.; Gershengorn, M.C. Seven transmembrane spanning receptors for free fatty acids as therapeutic targets for diabetes mellitus: pharmacological, phylogenetic and drug discovery aspects. J. Biol. Chem. 2008, 283(24), 16269-16273.
-
(2008)
J. Biol. Chem
, vol.283
, Issue.24
, pp. 16269-16273
-
-
Costanzi, S.1
Neumann, S.2
Gershengorn, M.C.3
-
12
-
-
79952825611
-
Free fatty acid receptors: Emerging targets for treatment of diabetes and its complications
-
Vangaveti, V.; Shashidhar, V.; Jarrod, G.; Baune, B.T.; Kennedy, R.L. Free fatty acid receptors: emerging targets for treatment of diabetes and its complications. Ther. Adv. Endocrinol. Metab., 2010, 1(4), 165-175
-
(2010)
Ther. Adv. Endocrinol. Metab
, vol.1
, Issue.4
, pp. 165-175
-
-
Vangaveti, V.1
Shashidhar, V.2
Jarrod, G.3
Baune, B.T.4
Kennedy, R.L.5
-
13
-
-
80955180014
-
Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders
-
Hara, T.; Hirasawa, A.; Ichimura, A.; Kimura, I.; Tsujimoto, G. Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders. J. Pharm. Sci., 2011, 100(9), 3594-3601.
-
(2011)
J. Pharm. Sci
, vol.100
, Issue.9
, pp. 3594-3601
-
-
Hara, T.1
Hirasawa, A.2
Ichimura, A.3
Kimura, I.4
Tsujimoto, G.5
-
14
-
-
80052684905
-
Experimental challenges to targeting poorly characterized GPCRs: Uncovering the therapeutic potential for free fatty acid receptors
-
Hudson, B.D.; Smith, N.J.; Milligan, G. Experimental challenges to targeting poorly characterized GPCRs: Uncovering the therapeutic potential for free fatty acid receptors. Adv. Pharmacol., 2011, 62, 175-218.
-
(2011)
Adv. Pharmacol
, vol.62
, pp. 175-218
-
-
Hudson, B.D.1
Smith, N.J.2
Milligan, G.3
-
15
-
-
80052021813
-
Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases
-
Talukdar, S.; Olefsky, J.M.; Osborn, O. Targeting GPR120 and other fatty acid-sensing GPCRs ameliorates insulin resistance and inflammatory diseases. Trends Pharmacol. Sci., 2011, 32(9), 543-50.
-
(2011)
Trends Pharmacol. Sci
, vol.32
, Issue.9
, pp. 543-550
-
-
Talukdar, S.1
Olefsky, J.M.2
Osborn, O.3
-
16
-
-
84872407744
-
Drug discovery opportunities and challenges at G protein coupled receptors for long chain free fatty acids
-
Holliday, N.D.; Watson, S.-J.; Brown, A.J.H. Drug discovery opportunities and challenges at G protein coupled receptors for long chain free fatty acids. Front. Endocrinol. 2:112.
-
Front. Endocrinol
, vol.2
, pp. 112
-
-
Holliday, N.D.1
Watson, S.-J.2
Brown, A.J.H.3
-
17
-
-
84874395887
-
Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets
-
Ulven, T. Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. Front. Endocrinol. 2012, 3, 111.
-
(2012)
Front. Endocrinol
, vol.3
, pp. 111
-
-
Ulven, T.1
-
18
-
-
80053138180
-
TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats
-
Tsujiha, Y.; Ito, R.; Suzuki, M.; Harada, A.; Negoro, N.; Yasuma, T.; Momose, Y.; Takeuchi, K. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J. Pharmacol. Exp. Ther., 2011, 339(1), 228-37.
-
(2011)
J. Pharmacol. Exp. Ther
, vol.339
, Issue.1
, pp. 228-237
-
-
Tsujiha, Y.1
Ito, R.2
Suzuki, M.3
Harada, A.4
Negoro, N.5
Yasuma, T.6
Momose, Y.7
Takeuchi, K.8
-
19
-
-
80555154306
-
AMG 837: A Novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents
-
Lin, D.C.; Zhang, J.; Zhuang, R.; Li, F.; Nguyen, K.; Chen, M.; Tran, T.; Lopez, E.; Lu, J.Y.; Li, X.N.; Tang, L.; Tonn, G.R.; Swaminath, G.; Reagan, J.D.; Chen, J.L.; Tian, H.; Lin, Y.J.; Houze, J.B.; Luo, J. AMG 837: A Novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One., 2011, 6(11), e27270.
-
(2011)
PLoS One
, vol.6
, Issue.11
-
-
Lin, D.C.1
Zhang, J.2
Zhuang, R.3
Li, F.4
Nguyen, K.5
Chen, M.6
Tran, T.7
Lopez, E.8
Lu, J.Y.9
Li, X.N.10
Tang, L.11
Tonn, G.R.12
Swaminath, G.13
Reagan, J.D.14
Chen, J.L.15
Tian, H.16
Lin, Y.J.17
Houze, J.B.18
Luo, J.19
-
20
-
-
84876720720
-
TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: A phase 2.; randomized.; double-blind.; placebo-controlled trial
-
Burant, C.F.; Viswanathan, P.; Marcinak, J.; Cao, C.; Vakilynejad, M.; Xie, B.; Leifke, E. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2.; randomized.; double-blind.; placebo-controlled trial. Lancet., 2012, 6736(11), 61879-61875.
-
(2012)
Lancet
, vol.6736
, Issue.11
, pp. 61875-61879
-
-
Burant, C.F.1
Viswanathan, P.2
Marcinak, J.3
Cao, C.4
Vakilynejad, M.5
Xie, B.6
Leifke, E.7
-
21
-
-
73649152457
-
Allosteric proteins and cellular control systems
-
Monod, J.; Changeux, J.P.; Jacob, F. Allosteric proteins and cellular control systems. J. Mol. Biol., 1963, 6, 306-329.
-
(1963)
J. Mol. Biol
, vol.6
, pp. 306-329
-
-
Monod, J.1
Changeux, J.P.2
Jacob, F.3
-
22
-
-
78651189765
-
On the nature of allosteric transitions: A plausible model
-
Monod, J.; Wyman, J.; Changeux, J.P. On the nature of allosteric transitions: a plausible model. J. Mol. Biol. 1965, 12, 88-118.
-
(1965)
J. Mol. Biol
, vol.12
, pp. 88-118
-
-
Monod, J.1
Wyman, J.2
Changeux, J.P.3
-
23
-
-
0036258990
-
G protein-coupled receptor allosterism and complexing
-
Christopoulos, A.; Kenakin, T. G protein-coupled receptor allosterism and complexing. Parmacol. Rev., 2002, 54(2), 323-374.
-
(2002)
Parmacol. Rev
, vol.54
, Issue.2
, pp. 323-374
-
-
Christopoulos, A.1
Kenakin, T.2
-
24
-
-
36448968578
-
Allosteric modulation of heterodimeric Gprotein-coupled receptors
-
Milligan, G.; Smith, N.J. Allosteric modulation of heterodimeric Gprotein-coupled receptors. Trends Pharmacol. Sci., 2007, 28(12), 615-620.
-
(2007)
Trends Pharmacol. Sci
, vol.28
, Issue.12
, pp. 615-620
-
-
Milligan, G.1
Smith, N.J.2
-
25
-
-
33847122495
-
Allosteric modulation of G protein-coupled receptors
-
May, L.T.; Leach, K.; Sexton, P.M.; Christopoulos, A. Allosteric modulation of G protein-coupled receptors. Annu. Rev. Pharmacol. Toxicol., 2007, 47, 1-51.
-
(2007)
Annu. Rev. Pharmacol. Toxicol
, vol.47
, pp. 1-51
-
-
May, L.T.1
Leach, K.2
Sexton, P.M.3
Christopoulos, A.4
-
26
-
-
58149193205
-
Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders
-
Conn, P.J.; Christopoulos, A.; Lindsley, C.W. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat. Rev. Drug Discov. 2009, 8(1), 41-54.
-
(2009)
Nat. Rev. Drug Discov
, vol.8
, Issue.1
, pp. 41-54
-
-
Conn, P.J.1
Christopoulos, A.2
Lindsley, C.W.3
-
27
-
-
78650147139
-
Allostery at G protein-coupled receptor homo-and heteromers: Uncharted pharmacological landscapes
-
Smith, N.J; Milligan, G. Allostery at G protein-coupled receptor homo-and heteromers: uncharted pharmacological landscapes. Pharmacol. Rev., 2010, 62(4), 701-725.
-
(2010)
Pharmacol. Rev
, vol.62
, Issue.4
, pp. 701-725
-
-
Smith, N.J.1
Milligan, G.2
-
28
-
-
84864462348
-
Allosteric modulators of rhodopsin-like G protein-coupled receptors: Opportunities in drug development
-
Müller, C.E.; Schiedel, A.C.; Baqi, Y. Allosteric modulators of rhodopsin-like G protein-coupled receptors: opportunities in drug development. Pharmacol. Ther., 2012, 135(3), 292-315.
-
(2012)
Pharmacol. Ther
, vol.135
, Issue.3
, pp. 292-315
-
-
Müller, C.E.1
Schiedel, A.C.2
Baqi, Y.3
-
29
-
-
24044539957
-
Allosteric modulation of the cannabinoid CB1 receptor
-
Price, M.R.; Baillie, G.L.; Thomas, A.; Stevenson, L.A.; Easson, M.; Goodwin, R.; McLean, A.; McIntosh, L.; Goodwin, G.; Walker, G.; Westwood, P.; Marrs, J.; Thomson, F.; Cowley, P.; Christopoulos, A.; Pertwee, R.G.; Ross, R.A. Allosteric modulation of the cannabinoid CB1 receptor. Mol. Pharmacol., 2005, 68(5), 1484-1495.
-
(2005)
Mol. Pharmacol
, vol.68
, Issue.5
, pp. 1484-1495
-
-
Price, M.R.1
Baillie, G.L.2
Thomas, A.3
Stevenson, L.A.4
Easson, M.5
Goodwin, R.6
McLean, A.7
McIntosh, L.8
Goodwin, G.9
Walker, G.10
Westwood, P.11
Marrs, J.12
Thomson, F.13
Cowley, P.14
Christopoulos, A.15
Pertwee, R.G.16
Ross, R.A.17
-
30
-
-
34447626644
-
GPCR functional selectivity has therapeutic impact
-
Mailman, R.B. GPCR functional selectivity has therapeutic impact. Trends Pharmacol. Sci., 2007, 28(8), 390-396.
-
(2007)
Trends Pharmacol. Sci
, vol.28
, Issue.8
, pp. 390-396
-
-
Mailman, R.B.1
-
31
-
-
73549098434
-
Ligand-and heterodimer-directed signaling of the CB(1) cannabinoid receptor
-
Hudson, B.D.; Hébert, T.E.; Kelly, M.E.M. Ligand-and heterodimer-directed signaling of the CB(1) cannabinoid receptor. Mol. Pharmacol., 2010, 77(1), 1-9.
-
(2010)
Mol. Pharmacol
, vol.77
, Issue.1
, pp. 1-9
-
-
Hudson, B.D.1
Hébert, T.E.2
Kelly, M.E.M.3
-
32
-
-
0029054965
-
Agonist-receptor efficacy. II. Agonist trafficking of receptor signals
-
Kenakin, T. Agonist-receptor efficacy. II. Agonist trafficking of receptor signals. Trends Pharmacol. Sci., 1995, 16(7), 232-238
-
(1995)
Trends Pharmacol. Sci
, vol.16
, Issue.7
, pp. 232-238
-
-
Kenakin, T.1
-
33
-
-
0035083109
-
Inverse, protean, and ligand-selective agonism: Matters of receptor conformation
-
Kenakin, T. Inverse, protean, and ligand-selective agonism: matters of receptor conformation. FASEB J., 2001, 15(3), 598-611.
-
(2001)
FASEB J
, vol.15
, Issue.3
, pp. 598-611
-
-
Kenakin, T.1
-
34
-
-
78650301416
-
When simple agonism is not enough: Emerging modalities of GPCR ligands
-
Smith, N.J.; Bennett, K.A.; Milligan, G. When simple agonism is not enough: emerging modalities of GPCR ligands. Mol. Cell. Endocrinol., 2011, 331(2), 241-247.
-
(2011)
Mol. Cell. Endocrinol
, vol.331
, Issue.2
, pp. 241-247
-
-
Smith, N.J.1
Bennett, K.A.2
Milligan, G.3
-
35
-
-
80053588007
-
Functional selectivity at the μ-opioid receptor: Implications for understanding opioid analgesia and tolerance
-
Raehal, K.M.; Schmid, C.L.; Groer, C.E.; Bohn, L.M. Functional selectivity at the μ-opioid receptor: implications for understanding opioid analgesia and tolerance. Pharmacol. Rev. 2011, 63(4), 1001-1019.
-
(2011)
Pharmacol. Rev
, vol.63
, Issue.4
, pp. 1001-1019
-
-
Raehal, K.M.1
Schmid, C.L.2
Groer, C.E.3
Bohn, L.M.4
-
36
-
-
0030693304
-
The benzodiazepine binding site of GABAA recepors
-
Sigel, E.; Buhr, A. The benzodiazepine binding site of GABAA recepors. Trends Pharmacol. Sci., 1997, 18, 425-429.
-
(1997)
Trends Pharmacol. Sci
, vol.18
, pp. 425-429
-
-
Sigel, E.1
Buhr, A.2
-
37
-
-
45749136445
-
Allosteric modulation of muscarinic acetylcholine receptors
-
Gregory, K.J.; Sexton, P.M.; Christopoulos A. Allosteric modulation of muscarinic acetylcholine receptors. Curr. Neuropharmacol., 2007, 5(3), 157-167.
-
(2007)
Curr. Neuropharmacol
, vol.5
, Issue.3
, pp. 157-167
-
-
Gregory, K.J.1
Sexton, P.M.2
Christopoulos, A.3
-
38
-
-
80052664751
-
Allosteric modulation of metabotropic glutamate receptors
-
Sheffler, D.J.; Gregory, K.J.; Rook, J.M.; Conn, P.J. Allosteric modulation of metabotropic glutamate receptors. Adv. Pharmacol. 2011, 62, 37-77.
-
(2011)
Adv. Pharmacol
, vol.62
, pp. 37-77
-
-
Sheffler, D.J.1
Gregory, K.J.2
Rook, J.M.3
Conn, P.J.4
-
39
-
-
84867306794
-
Identification and pharmacological characterization of multiple allosteric binding sites on the free Fatty Acid 1 receptor
-
Lin, D.C.; Guo, Q.; Luo, J.; Zhang, J.; Nguyen, K.; Chen, M.; Tran, T.; Dransfield, P.J.; Brown, S.P.; Houze, J.; Vimolratana, M.; Jiao, X.Y.; Wang, Y.; Birdsall, N.J.; Swaminath, G. Identification and pharmacological characterization of multiple allosteric binding sites on the free Fatty Acid 1 receptor. Mol. Pharmacol., 2012, 82(5), 843-859.
-
(2012)
Mol. Pharmacol
, vol.82
, Issue.5
, pp. 843-859
-
-
Lin, D.C.1
Guo, Q.2
Luo, J.3
Zhang, J.4
Nguyen, K.5
Chen, M.6
Tran, T.7
Dransfield, P.J.8
Brown, S.P.9
Houze, J.10
Vimolratana, M.11
Jiao, X.Y.12
Wang, Y.13
Birdsall, N.J.14
Swaminath, G.15
-
40
-
-
0034604451
-
Crystal structure of rhodopsin: A G protein-coupled receptor
-
Palczewski, K.; Kumasaka, T.; Hori, T.; Behnke, C.A.; Motoshima, H.; Fox, B.A.; Le Trong, I.; Teller, D.C.; Okada, T.; Stenkamp, R.E.; Yamamoto, M.; Miyano, M. Crystal structure of rhodopsin: A G protein-coupled receptor. Science. 2000, 289(5480), 739-745.
-
(2000)
Science
, vol.289
, Issue.5480
, pp. 739-745
-
-
Palczewski, K.1
Kumasaka, T.2
Hori, T.3
Behnke, C.A.4
Motoshima, H.5
Fox, B.A.6
Le Trong, I.7
Teller, D.C.8
Okada, T.9
Stenkamp, R.E.10
Yamamoto, M.11
Miyano, M.12
-
41
-
-
36248970132
-
Crystal structure of the human beta2 adrenergic G-proteincoupled receptor
-
Rasmussen, S.G.; Choi, H.J.; Rosenbaum, D.M.; Kobilka, T.S.; Thian, F.S.; Edwards, P.C.; Burghammer, M.; Ratnala, V.R.; Sanishvili, R.; Fischetti, R.F.; Schertler, G.F.; Weis, W.I.; Kobilka, B.K. Crystal structure of the human beta2 adrenergic G-proteincoupled receptor. Nature, 2007, 450(7168), 383-287.
-
(2007)
Nature
, vol.450
, Issue.7168
, pp. 287-383
-
-
Rasmussen, S.G.1
Choi, H.J.2
Rosenbaum, D.M.3
Kobilka, T.S.4
Thian, F.S.5
Edwards, P.C.6
Burghammer, M.7
Ratnala, V.R.8
Sanishvili, R.9
Fischetti, R.F.10
Schertler, G.F.11
Weis, W.I.12
Kobilka, B.K.13
-
42
-
-
47949129742
-
Structure of a beta1-adrenergic G-protein-coupled receptor
-
Warne, T.; Serrano-Vega, M.J.; Baker, J.G.; Moukhametzianov, R.; Edwards, P.C.; Henderson, R.; Leslie, A.G.; Tate, C.G.; Schertler, G.F. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature, 2008, 454(7203), 486-491.
-
(2008)
Nature
, vol.454
, Issue.7203
, pp. 486-491
-
-
Warne, T.1
Serrano-Vega, M.J.2
Baker, J.G.3
Moukhametzianov, R.4
Edwards, P.C.5
Henderson, R.6
Leslie, A.G.7
Tate, C.G.8
Schertler, G.F.9
-
43
-
-
56749103466
-
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist
-
Jaakola, V.P.; Griffith, M.T.; Hanson, M.A.; Cherezov, V.; Chien, E.Y.; Lane, J.R.; Ijzerman, A.P.; Stevens, R.C. The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science, 2008, 322(5905), 1211-1217.
-
(2008)
Science
, vol.322
, Issue.5905
, pp. 1211-1217
-
-
Jaakola, V.P.1
Griffith, M.T.2
Hanson, M.A.3
Cherezov, V.4
Chien, E.Y.5
Lane, J.R.6
Ijzerman, A.P.7
Stevens, R.C.8
-
44
-
-
80051658642
-
Crystal structure of the β2 adrenergic receptor-Gs protein complex
-
Rasmussen, S.G.; DeVree, B.T.; Zou, Y.; Kruse, A.C.; Chung, K.Y.; Kobilka, T.S.; Thian, F.S.; Chae, P.S.; Pardon, E.; Calinski, D.; Mathiesen, J.M.; Shah, S.T.; Lyons, J.A.; Caffrey, M.; Gellman, S.H.; Steyaert, J.; Skiniotis, G.; Weis, W.I.; Sunahara, R.K.; Kobilka, B.K. Crystal structure of the β2 adrenergic receptor-Gs protein complex. Nature, 2011, 477(7366), 549-555.
-
(2011)
Nature
, vol.477
, Issue.7366
, pp. 549-555
-
-
Rasmussen, S.G.1
Devree, B.T.2
Zou, Y.3
Kruse, A.C.4
Chung, K.Y.5
Kobilka, T.S.6
Thian, F.S.7
Chae, P.S.8
Pardon, E.9
Calinski, D.10
Mathiesen, J.M.11
Shah, S.T.12
Lyons, J.A.13
Caffrey, M.14
Gellman, S.H.15
Steyaert, J.16
Skiniotis, G.17
Weis, W.I.18
Sunahara, R.K.19
Kobilka, B.K.20
more..
-
45
-
-
84861075468
-
Structure of the δ-opioid receptor bound to naltrindole
-
Granier, S.; Manglik, A.; Kruse, AC.; Kobilka, T.S.; Thian, F.S.; Weis, W.I.; Kobilka, B.K. Structure of the δ-opioid receptor bound to naltrindole. Nature. 2012, 485(7398), 400-404.
-
(2012)
Nature
, vol.485
, Issue.7398
, pp. 400-404
-
-
Granier, S.1
Manglik, A.2
Kruse, A.C.3
Kobilka, T.S.4
Thian, F.S.5
Weis, W.I.6
Kobilka, B.K.7
-
46
-
-
84857254248
-
Crystal structure of a lipid G protein-coupled receptor
-
Hanson, M.A.; Roth, C.B.; Jo, E.; Griffith, M.T.; Scott, F.L.; Reinhart, G.; Desale, H.; Clemons, B.; Cahalan, S.M.; Schuerer, S.C.; Sanna, M.G.; Han, G.W.; Kuhn, P.; Rosen, H.; Stevens, R.C. Crystal structure of a lipid G protein-coupled receptor. Science, 2012, 335(6070), 851-855.
-
(2012)
Science
, vol.335
, Issue.6070
, pp. 851-855
-
-
Hanson, M.A.1
Roth, C.B.2
Jo, E.3
Griffith, M.T.4
Scott, F.L.5
Reinhart, G.6
Desale, H.7
Clemons, B.8
Cahalan, S.M.9
Schuerer, S.C.10
Sanna, M.G.11
Han, G.W.12
Kuhn, P.13
Rosen, H.14
Stevens, R.C.15
-
47
-
-
84861096654
-
Crystal structure of the μ-opioid receptor bound to a morphinan antagonist
-
Manglik, A.; Kruse, A.C.; Kobilka, T.S.; Thian, F.S.; Mathiesen, J.M.; Sunahara, R.K.; Pardo, L.; Weis, W.I.; Kobilka, B.K.; Granier, S. Crystal structure of the μ-opioid receptor bound to a morphinan antagonist. Nature., 2012, 485(7398), 321-326.
-
(2012)
Nature
, vol.485
, Issue.7398
, pp. 321-326
-
-
Manglik, A.1
Kruse, A.C.2
Kobilka, T.S.3
Thian, F.S.4
Mathiesen, J.M.5
Sunahara, R.K.6
Pardo, L.7
Weis, W.I.8
Kobilka, B.K.9
Granier, S.10
-
48
-
-
84870290491
-
Structure of the chemokine receptor CXCR1 in phospholipid bilayers
-
Park, S.H.; Das, B.B.; Casagrande, F.; Tian, Y.; Nothnagel, H.J.; Chu, M.; Kiefer, H.; Maier, K.; De Angelis, A.A.; Marassi, F.M.; Opella, S.J. Structure of the chemokine receptor CXCR1 in phospholipid bilayers. Nature, 2012, 491(7426), 779-783.
-
(2012)
Nature
, vol.491
, Issue.7426
, pp. 779-783
-
-
Park, S.H.1
Das, B.B.2
Casagrande, F.3
Tian, Y.4
Nothnagel, H.J.5
Chu, M.6
Kiefer, H.7
Maier, K.8
de Angelis, A.A.9
Marassi, F.M.10
Opella, S.J.11
-
49
-
-
84861019261
-
Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic
-
Thompson, A.A; Liu, W.; Chun, E.; Katritch, V.; Wu, H.; Vardy, E.; Huang, X.P.; Trapella, C.; Guerrini, R.; Calo, G.; Roth, B.L.; Cherezov, V.; Stevens, R.C. Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature, 2012, 485(7398), 395-399.
-
(2012)
Nature
, vol.485
, Issue.7398
, pp. 395-399
-
-
Thompson, A.A.1
Liu, W.2
Chun, E.3
Katritch, V.4
Wu, H.5
Vardy, E.6
Huang, X.P.7
Trapella, C.8
Guerrini, R.9
Calo, G.10
Roth, B.L.11
Cherezov, V.12
Stevens, R.C.13
-
50
-
-
84858110277
-
Homology modeling of class a G protein-coupled receptors
-
Costanzi, S. Homology modeling of class a G protein-coupled receptors. Methods Mol. Biol. 2012, 857, 259-279.
-
(2012)
Methods Mol. Biol
, vol.857
, pp. 259-279
-
-
Costanzi, S.1
-
51
-
-
84865201339
-
Homology model-assisted elucidation of binding sites in GPCRs
-
Levit, A.; Barak, D.; Behrens, M.; Meyerhof, W.; Niv, MY. Homology model-assisted elucidation of binding sites in GPCRs. Methods Mol. Biol., 2012, 914, 179-205.
-
(2012)
Methods Mol. Biol
, vol.914
, pp. 179-205
-
-
Levit, A.1
Barak, D.2
Behrens, M.3
Meyerhof, W.4
Niv, M.Y.5
-
52
-
-
34548476934
-
Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G proteincoupled receptors ligands
-
Avlani, V.A.; Gregory, K.J.; Morton, C.J.; Parker, M.W.; Sexton, P.M.; Cristopoulos, A. Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G proteincoupled receptors ligands. J. Biol. Chem., 2007, 282, 25677-25686.
-
(2007)
J. Biol. Chem
, vol.282
, pp. 25677-25686
-
-
Avlani, V.A.1
Gregory, K.J.2
Morton, C.J.3
Parker, M.W.4
Sexton, P.M.5
Cristopoulos, A.6
-
53
-
-
84860671694
-
The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation
-
Peeters, M.C.; Wisse, L.E.; Dinaj, A.; Vroling, B.; Vriend, G.; Ijzerman, A.P. The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation. Biochem. Pharmacol., 2012, 84(1), 76-87.
-
(2012)
Biochem. Pharmacol
, vol.84
, Issue.1
, pp. 76-87
-
-
Peeters, M.C.1
Wisse, L.E.2
Dinaj, A.3
Vroling, B.4
Vriend, G.5
Ijzerman, A.P.6
-
54
-
-
40849124250
-
An intracellular allosteric site for a specific class of antagonists of the CC chemokine G protein-coupled receptors CCR4 and CCR5
-
Andrews, G.; Jones, C.; Wreggett, K.A. An intracellular allosteric site for a specific class of antagonists of the CC chemokine G protein-coupled receptors CCR4 and CCR5. Mol. Pharmacol., 2008, 73, 855-867.
-
(2008)
Mol. Pharmacol
, vol.73
, pp. 855-867
-
-
Andrews, G.1
Jones, C.2
Wreggett, K.A.3
-
55
-
-
79952600213
-
Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1
-
Dowal, L.; Sim, D.S.; Dilks, J.R.; Blair, P.; Beaudry, S.; Denker, B.M.; Koukos, G.; Kuliopulos, A.; Flaumenhaft, R. Identification of an antithrombotic allosteric modulator that acts through helix 8 of PAR1. Proc. Nat. Acad. Sci. U.S.A., 2011, 108(7), 2951-2956.
-
(2011)
Proc. Nat. Acad. Sci. U.S.A
, vol.108
, Issue.7
, pp. 2951-2956
-
-
Dowal, L.1
Sim, D.S.2
Dilks, J.R.3
Blair, P.4
Beaudry, S.5
Denker, B.M.6
Koukos, G.7
Kuliopulos, A.8
Flaumenhaft, R.9
-
56
-
-
84455173446
-
Probe dependence in the allosteric modulation of a G protein-coupled receptor: Implications for detection and validation of allosteric ligand effects
-
Valant, C.; Felder, C.C.; Sexton, P.M.; Christopoulos, A. Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects. Mol. Pharmacol., 2012, 81(1), 41-52.
-
(2012)
Mol. Pharmacol
, vol.81
, Issue.1
, pp. 41-52
-
-
Valant, C.1
Felder, C.C.2
Sexton, P.M.3
Christopoulos, A.4
-
57
-
-
79953899942
-
Allosteric modulation of family C G-protein-coupled receptors: From molecular insights to therapeutic perspectives
-
Urwyler, S. Allosteric modulation of family C G-protein-coupled receptors: from molecular insights to therapeutic perspectives. Pharmacol. Rev., 2011, 63(1), 59-126.
-
(2011)
Pharmacol. Rev
, vol.63
, Issue.1
, pp. 59-126
-
-
Urwyler, S.1
-
58
-
-
84863635488
-
M1 muscarinic acetylcholine receptor allosteric modulators as potential therapeutics opportunities for treating Alzheimer's disease
-
Decker, M.; Holzgrabe, U. M1 muscarinic acetylcholine receptor allosteric modulators as potential therapeutics opportunities for treating Alzheimer's disease. Med. Chem. Commun., 2012, 3(7), 752-762.
-
(2012)
Med. Chem. Commun
, vol.3
, Issue.7
, pp. 752-762
-
-
Decker, M.1
Holzgrabe, U.2
-
59
-
-
33846936284
-
Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA
-
Zhao, Z.; Wisnoski, D.D.; O'Brien, J.A.; Lemaire, W.; Williams, D.L, Jr.; Jacobson, M.A.; Wittman, M.; Ha, S.N.; Schaffhauser, H.; Sur, C.; Pettibone, D.J.; Duggan, M.E.; Conn, P.J.; Hartman, G.D.; Lindsley, C.W. Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. Bioorg. Med. Chem. Lett., 2007, 17(5), 1386-1391.
-
(2007)
Bioorg. Med. Chem. Lett
, vol.17
, Issue.5
, pp. 1386-1391
-
-
Zhao, Z.1
Wisnoski, D.D.2
O'Brien, J.A.3
Lemaire, W.4
Williams Jr., D.L.5
Jacobson, M.A.6
Wittman, M.7
Ha, S.N.8
Schaffhauser, H.9
Sur, C.10
Pettibone, D.J.11
Duggan, M.E.12
Conn, P.J.13
Hartman, G.D.14
Lindsley, C.W.15
-
60
-
-
79953213637
-
Molecular switches on mGluR allosteric ligands that modulate modes of pharmacology
-
Wood, M.R.; Hopkins, C.R.; Brogan, J.T.; Conn, P.J.; Lindsley, C.W. Molecular switches on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry. 2011, 50(13), 2403-10.
-
(2011)
Biochemistry
, vol.50
, Issue.13
, pp. 2403-2410
-
-
Wood, M.R.1
Hopkins, C.R.2
Brogan, J.T.3
Conn, P.J.4
Lindsley, C.W.5
-
61
-
-
77953845365
-
Key considerations around the risks and consequences of hypoglycaemia in people with type 2 diabetes
-
Barnett, A.H.; Cradock, S.; Fisher, M.; Hall, G.; Hughes, E.; Middleton, A. Key considerations around the risks and consequences of hypoglycaemia in people with type 2 diabetes. Int. J. Clin. Pract. 2010, 64(8), 1121-1129.
-
(2010)
Int. J. Clin. Pract
, vol.64
, Issue.8
, pp. 1121-1129
-
-
Barnett, A.H.1
Cradock, S.2
Fisher, M.3
Hall, G.4
Hughes, E.5
Middleton, A.6
-
62
-
-
33745607930
-
Pharmacolgical regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: Identification of agonist and antagonist small molecules
-
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. Pharmacolgical 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(5), 619-628.
-
(2006)
Br. J. Pharmacol
, vol.148
, Issue.5
, pp. 619-628
-
-
Briscoe, C.P.1
Peat, A.J.2
McKeown, S.C.3
Corbett, D.F.4
Goetz, A.S.5
Littleton, T.R.6
McCoy, D.C.7
Kenakin, T.P.8
Andrews, J.L.9
Ammala, C.10
Fornwald, J.A.11
Ignar, D.M.12
Jenkinson, S.13
-
63
-
-
56749163623
-
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
-
Christiansen, E.; Urban, C.; Merten, N.; Liebscher, K.; Karlsen, K.K.; Hamacher, A.; Spinrath, A.; Bond, A.D.; Drewke, C.; Ullrich, S.; Kassack, M.U.; Kostenis, E.; Ulven, T. 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. J. Med. Chem., 2008, 51(22), 7061-7064.
-
(2008)
J. Med. Chem
, vol.51
, Issue.22
, pp. 7061-7064
-
-
Christiansen, E.1
Urban, C.2
Merten, N.3
Liebscher, K.4
Karlsen, K.K.5
Hamacher, A.6
Spinrath, A.7
Bond, A.D.8
Drewke, C.9
Ullrich, S.10
Kassack, M.U.11
Kostenis, E.12
Ulven, T.13
-
64
-
-
50949128408
-
Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice
-
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(8), 2211-2219.
-
(2008)
Diabetes
, vol.57
, Issue.8
, pp. 2211-2219
-
-
Tan, C.P.1
Feng, Y.2
Zhou, Y.P.3
Eiermann, G.J.4
Petrov, A.5
Zhou, C.6
Lin, S.7
Salituro, G.8
Meinke, P.9
Mosley, R.10
Akiyama, T.E.11
Einstein, M.12
Kumar, S.13
Berger, J.P.14
Mills, S.G.15
Thornberry, N.A.16
Yang, L.17
Howard, A.D.18
-
65
-
-
67649331670
-
Progress in the discovery and development of small-molecule modulators of Gprotein-coupled receptor 40 (GPR40/FFA1/FFAR1): An emerging target for type 2 diabetes
-
Bharate, S.B.; Nemmani, K.V.S.; Vishwakarma, R.A. Progress in the discovery and development of small-molecule modulators of Gprotein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes. Expert Opin. Ther. Patents., 2009, 19(2), 237-264.
-
(2009)
Expert Opin. Ther. Patents
, vol.19
, Issue.2
, pp. 237-264
-
-
Bharate, S.B.1
Nemmani, K.V.S.2
Vishwakarma, R.A.3
-
66
-
-
77956500937
-
Discovery of TAK-875: A potent, selective and orally bioavailable GPR40 agonist
-
Negoro, N.; Sasaki, S.; Mikami, S.; Ito, M.; Suzuki, M.; Tsujihata, Y.; Ito, R.; Harada, A.; Takeuchi, K.; Suzuki, N.; Miyazaki, J.; Santou, T.; Odani, T.; Kanzaki, N.; Funami, M.; Tanaka, T.; Kogame, A.; Matsunaga, S.; Yasuma, T.; Momose, Y. Discovery of TAK-875: a potent, selective and orally bioavailable GPR40 agonist. Med. Chem. Lett., 2010, 1, 290-294.
-
(2010)
Med. Chem. Lett
, vol.1
, pp. 290-294
-
-
Negoro, N.1
Sasaki, S.2
Mikami, S.3
Ito, M.4
Suzuki, M.5
Tsujihata, Y.6
Ito, R.7
Harada, A.8
Takeuchi, K.9
Suzuki, N.10
Miyazaki, J.11
Santou, T.12
Odani, T.13
Kanzaki, N.14
Funami, M.15
Tanaka, T.16
Kogame, A.17
Matsunaga, S.18
Yasuma, T.19
Momose, Y.20
more..
-
67
-
-
80053910894
-
Identification of a potent and selective free fatty acid rReceptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME Properties
-
Christiansen, E.; Urban, C.; Grundmann, M.; Due-Hansen, M.E.; Hagesaether, E.; Schmidt, J.; Pardo, L.; Ullrich, S.; Kostenis, E.; Kassack, M.: Ulven, T. Identification of a potent and selective free fatty acid rReceptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME Properties. J. Med. Chem., 2011, 54(19), 6691-6703.
-
(2011)
J. Med. Chem
, vol.54
, Issue.19
, pp. 6691-6703
-
-
Christiansen, E.1
Urban, C.2
Grundmann, M.3
Due-Hansen, M.E.4
Hagesaether, E.5
Schmidt, J.6
Pardo, L.7
Ullrich, S.8
Kostenis, E.9
Kassack, M.10
Ulven, T.11
-
68
-
-
84864228135
-
Free fatty acid receptor 1 (FFA1/GPR40) agonists: Mesylpropoxy appendage lowers lipophilicity and improves ADME properties
-
Christiansen, E.; Due-Hansen, M.E.; Urban, C.; Grundmann, M.; Schröder, R.; Hudson, B.D.; Milligan, G.; Cawthorne, M.A.; Kostenis, E.; Kassack, M.U.; Ulven, T. Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties. J. Med. Chem. 2012, 55(14), 6624-6628.
-
(2012)
J. Med. Chem
, vol.55
, Issue.14
, pp. 6624-6628
-
-
Christiansen, E.1
Due-Hansen, M.E.2
Urban, C.3
Grundmann, M.4
Schröder, R.5
Hudson, B.D.6
Milligan, G.7
Cawthorne, M.A.8
Kostenis, E.9
Kassack, M.U.10
Ulven, T.11
-
69
-
-
34347220548
-
Bidirectional.; iterative approach to the structural delineation of the functional chemoprint in GPR40 for agonist recognition
-
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(13), 2981-2989.
-
(2007)
J. Med. Chem
, vol.50
, Issue.13
, pp. 2981-2989
-
-
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
-
70
-
-
35748937333
-
Identification of residues important for agonist recognition and activation in GPR40
-
Sum, C.S.; Tikhonova, I.G.; Neumann, S.; Engel, S.; Raaka, B.M.; Costanzi, S.; Gershengorn, M.C. Identification of residues important for agonist recognition and activation in GPR40. J. Biol. Chem., 2007, 282(40), 29248-29255.
-
(2007)
J. Biol. Chem
, vol.282
, Issue.40
, pp. 29248-29255
-
-
Sum, C.S.1
Tikhonova, I.G.2
Neumann, S.3
Engel, S.4
Raaka, B.M.5
Costanzi, S.6
Gershengorn, M.C.7
-
71
-
-
0037423719
-
A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs
-
Kotarsky, K.; Nilsson, N.E.; Flodgren, E.; Owman, C.; Olde, B. A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs. Biochem. Biophys. Res. Commun., 2003, 301(2), 406-410.
-
(2003)
Biochem. Biophys. Res. Commun
, vol.301
, Issue.2
, pp. 406-410
-
-
Kotarsky, K.1
Nilsson, N.E.2
Flodgren, E.3
Owman, C.4
Olde, B.5
-
72
-
-
67650533801
-
The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1
-
Smith, N.J.; Stoddart, L.A.; Devine, N.M.; Jenkins, L.; Milligan, G. The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1. J. Biol. Chem., 2009, 284(26), 17527-17539.
-
(2009)
J. Biol. Chem
, vol.284
, Issue.26
, pp. 17527-17539
-
-
Smith, N.J.1
Stoddart, L.A.2
Devine, N.M.3
Jenkins, L.4
Milligan, G.5
-
73
-
-
84867290314
-
A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents
-
Luo, J.; Swaminath, G.; Brown, S.P.; Zhang, J.; Guo, Q.; Chen, M.; Nguyen, K.; Tran, T.; Miao, L.; Dransfield, P.J.; Vimolratana, M.; Houze, J.B.; Wong, S.; Toteva, M.; Shan, B.; Li, F.; Zhuang, R.; Lin, D.C. A Potent Class of GPR40 Full Agonists Engages the EnteroInsular Axis to Promote Glucose Control in Rodents. PLoS One, 2012, 7(10), e46300.
-
(2012)
PLoS One
, vol.7
, Issue.10
-
-
Luo, J.1
Swaminath, G.2
Brown, S.P.3
Zhang, J.4
Guo, Q.5
Chen, M.6
Nguyen, K.7
Tran, T.8
Miao, L.9
Dransfield, P.J.10
Vimolratana, M.11
Houze, J.B.12
Wong, S.13
Toteva, M.14
Shan, B.15
Li, F.16
Zhuang, R.17
Lin, D.C.18
-
74
-
-
52749098923
-
GPR40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion
-
Edfalk, S.; Steneberg, P.; Edlund, H. GPR40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes, 2008, 57(9), 2280-2287.
-
(2008)
Diabetes
, vol.57
, Issue.9
, pp. 2280-2287
-
-
Edfalk, S.1
Steneberg, P.2
Edlund, H.3
-
75
-
-
0014215242
-
Hypoglycaemia and hyperinsulinaemia in response to raised free-fatty-acid levels
-
Greenough, W.B.; Crespin, S.R.; Steinberg, D. Hypoglycaemia and hyperinsulinaemia in response to raised free-fatty-acid levels. Lancet, 1967, 2(7530), 1334-1336.
-
(1967)
Lancet
, vol.2
, Issue.7530
, pp. 1334-1336
-
-
Greenough, W.B.1
Crespin, S.R.2
Steinberg, D.3
-
76
-
-
0042922453
-
Saturated Fatty Acids Synergize with Elevated Glucose to Cause Pancreatic β-Cell Death
-
El-Assaad, W.; Buteau, J.; Peyot, M.L.; Nolan, C.; Roduit, R.; Hardy, S.; Joly, E.; Dbaibo, G.; Rosenberg, L.; Prentki, M. Saturated Fatty Acids Synergize with Elevated Glucose to Cause Pancreatic β-Cell Death. Endocrinology, 2003, 144(9), 4154-4163.
-
(2003)
Endocrinology
, vol.144
, Issue.9
, pp. 4154-4163
-
-
El-Assaad, W.1
Buteau, J.2
Peyot, M.L.3
Nolan, C.4
Roduit, R.5
Hardy, S.6
Joly, E.7
Dbaibo, G.8
Rosenberg, L.9
Prentki, M.10
-
77
-
-
20944433543
-
The FFA receptor GPR40 links hyperinsulinemia.; hepatic steatosis.; and impaired glucose homeostasis in mouse
-
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(4), 245-258.
-
(2005)
Cell Metab
, vol.1
, Issue.4
, pp. 245-258
-
-
Steneberg, P.1
Rubins, N.2
Bartoov-Shifman, R.3
Walker, M.D.4
Edlund, H.5
-
78
-
-
70350309324
-
Lipid receptors and islet function: Therapeutic implicaitons?
-
Kebede, M.A.; Alquier, T.; Latour, M.G.; Poitout, V. Lipid receptors and islet function: therapeutic implicaitons? Diabetes Obes. Metab., 2009, 11(Suppl 4), 10-20.
-
(2009)
Diabetes Obes. Metab
, vol.11
, Issue.SUPPL. 4
, pp. 10-20
-
-
Kebede, M.A.1
Alquier, T.2
Latour, M.G.3
Poitout, V.4
-
79
-
-
58149100292
-
Lack of FFAR1/GPR40 does not protect mice from high-fat dietinduced metabolic disease
-
Lan, H.; Hoos, L.M.; Liu, L.; Tetzloff, G.; Hu, W.; Abbondanzo, S.J.; Vassileva, G.; Gustafson, E.L.; Hedrick, J.A.; Davis, H.R. Lack of FFAR1/GPR40 does not protect mice from high-fat dietinduced metabolic disease. Diabetes, 2008, 57(11), 2999-3006.
-
(2008)
Diabetes
, vol.57
, Issue.11
, pp. 2999-3006
-
-
Lan, H.1
Hoos, L.M.2
Liu, L.3
Tetzloff, G.4
Hu, W.5
Abbondanzo, S.J.6
Vassileva, G.7
Gustafson, E.L.8
Hedrick, J.A.9
Davis, H.R.10
-
80
-
-
84873835561
-
Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes
-
Kaku, K.; Araki, T.; Yoshinaka, R. Randomized, double-blind, dose-ranging study of TAK-875, a novel GPR40 agonist, in Japanese patients with inadequately controlled type 2 diabetes. Diabetes Care, 2013, 36(2), 245-250.
-
(2013)
Diabetes Care
, vol.36
, Issue.2
, pp. 245-250
-
-
Kaku, K.1
Araki, T.2
Yoshinaka, R.3
-
81
-
-
79953216793
-
Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: Identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3
-
Schmidt, J.; Smith, N.J.; Christiansen, E.; Tikhonova, I.G.; Grundmann, M.; Hudson, B.D.; Ward, R.J.; 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. J Biol Chem., 2011, 286(12), 10628-10640.
-
(2011)
J Biol Chem
, vol.286
, Issue.12
, pp. 10628-10640
-
-
Schmidt, J.1
Smith, N.J.2
Christiansen, E.3
Tikhonova, I.G.4
Grundmann, M.5
Hudson, B.D.6
Ward, R.J.7
Drewke, C.8
Milligan, G.9
Kostenis, E.10
Ulven, T.11
-
82
-
-
84870373974
-
Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs
-
Hudson, B.D.; Christiansen, E.; Tikhonova, I.G.; Grundmann, M.; Kostenis, E.; Adams, D.R.; Ulven, T.; Milligan, G. Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs. FASEB J., 2012, 26(12), 4951-4965.
-
(2012)
FASEB J
, vol.26
, Issue.12
, pp. 4951-4965
-
-
Hudson, B.D.1
Christiansen, E.2
Tikhonova, I.G.3
Grundmann, M.4
Kostenis, E.5
Adams, D.R.6
Ulven, T.7
Milligan, G.8
-
83
-
-
84870361150
-
Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3
-
Hudson, B.D.; Tikhonova, I.G.; Pandey, S.K.; 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. J. Biol. Chem., 2012, 287(49), 41195-411209.
-
(2012)
J. Biol. Chem
, vol.287
, Issue.49
, pp. 41195-411209
-
-
Hudson, B.D.1
Tikhonova, I.G.2
Pandey, S.K.3
Ulven, T.4
Milligan, G.5
-
84
-
-
57749112018
-
Conserved polar residues in transmembrane domains V.; VI.; and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids
-
Stoddart, L.A.; Smith, N.J.; Jenkins, L.; Brown, A.J.; Milligan, G. Conserved polar residues in transmembrane domains V.; VI.; and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids. J. Biol. Chem., 2008, 283(47), 32913-32924.
-
(2008)
J. Biol. Chem
, vol.283
, Issue.47
, pp. 32913-32924
-
-
Stoddart, L.A.1
Smith, N.J.2
Jenkins, L.3
Brown, A.J.4
Milligan, G.5
-
85
-
-
84876696141
-
-
International patent Application, WO 2010/066682, June 17
-
Hoveyda, H.; Brantis, C.E.; Dutheuil, G.; Zoute, L.; Schils, D.; Bernard, J. Compounds, pharmaceutical composition and methods for use in treating metabolic disorders. International patent Application, WO 2010/066682, June 17, 2010.
-
(2010)
Compounds, Pharmaceutical Composition and Methods For Use In Treating Metabolic Disorders
-
-
Hoveyda, H.1
Brantis, C.E.2
Dutheuil, G.3
Zoute, L.4
Schils, D.5
Bernard, J.6
-
86
-
-
84864570952
-
-
International patent application, WO/2011/092284, August 4
-
Brantis, C.E.; Ooms, F.; Bernard, J. Novel amino acid derivatives and their use as GPR43 receptor modulators. International patent application, WO/2011/092284, August 4, 2011.
-
(2011)
Novel Amino Acid Derivatives and Their Use As GPR43 Receptor Modulators
-
-
Brantis, C.E.1
Ooms, F.2
Bernard, J.3
-
87
-
-
57349142454
-
Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2
-
Lee, T.; Schwandner, R.; Swaminath, G.; Weiszmann, J.; Cardozo, M.; Greenberg, J.; Jaeckel, P.; Ge, H.; Wang, Y.; Jiao, X.; Liu, J.; Kayser, F.; Tian, H.; Li, Y. Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2. Mol. Pharmacol., 2008, 74(6), 1599-1609.
-
(2008)
Mol. Pharmacol
, vol.74
, Issue.6
, pp. 1599-1609
-
-
Lee, T.1
Schwandner, R.2
Swaminath, G.3
Weiszmann, J.4
Cardozo, M.5
Greenberg, J.6
Jaeckel, P.7
Ge, H.8
Wang, Y.9
Jiao, X.10
Liu, J.11
Kayser, F.12
Tian, H.13
Li, Y.14
-
88
-
-
72249086955
-
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators
-
Wang, Y.; Jiao, X.; Kayser, F.; Liu, J.; Wang, Z.; Wanska, M.; Greenberg, J.; Weiszmann, J.; Ge, H.; Tian, H.; Wong, S.; Schwandner, R.; Lee, T.; Li, Y. The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators. Bioorg. Med. Chem. Lett., 2010, 20(2), 493-498.
-
(2010)
Bioorg. Med. Chem. Lett
, vol.20
, Issue.2
, pp. 493-498
-
-
Wang, Y.1
Jiao, X.2
Kayser, F.3
Liu, J.4
Wang, Z.5
Wanska, M.6
Greenberg, J.7
Weiszmann, J.8
Ge, H.9
Tian, H.10
Wong, S.11
Schwandner, R.12
Lee, T.13
Li, Y.14
-
89
-
-
79959309348
-
Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator
-
Smith, N.J.; Ward, R.J.; Stoddart, L.A.; Hudson, B.D.; Kostenis, E.; Ulven, T.; Morris, J.C.; Tränkle, C.; Tikhonova, I.G.; Adams, D.R.; Milligan G. Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Mol. Pharmacol., 2011, 80(1), 163-173.
-
(2011)
Mol. Pharmacol
, vol.80
, Issue.1
, pp. 163-173
-
-
Smith, N.J.1
Ward, R.J.2
Stoddart, L.A.3
Hudson, B.D.4
Kostenis, E.5
Ulven, T.6
Morris, J.C.7
Tränkle, C.8
Tikhonova, I.G.9
Adams, D.R.10
Milligan, G.11
-
90
-
-
69249214021
-
Agonism and allosterism: The pharmacology of the free fatty acid receptors FFA2 and FFA3
-
Milligan, G.; Stoddart, L.A.; Smith, N.J. Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3. Br. J. Pharmacol., 2009, 158(1), 146-153.
-
(2009)
Br. J. Pharmacol
, vol.158
, Issue.1
, pp. 146-153
-
-
Milligan, G.1
Stoddart, L.A.2
Smith, N.J.3
-
91
-
-
79551491907
-
Mutational analysis of G-protein coupled receptor-FFA2
-
Swaminath, G.; Jaeckel, P.; Guo, Q.; Cardozo, M.; Weiszmann, J.; Lindberg, R.; Wang, Y.; Schwandner, R.; Li, Y. Mutational analysis of G-protein coupled receptor-FFA2. Biochem. Biophys. Res. Commun., 2011, 405(1), 122-127.
-
(2011)
Biochem. Biophys. Res. Commun
, vol.405
, Issue.1
, pp. 122-127
-
-
Swaminath, G.1
Jaeckel, P.2
Guo, Q.3
Cardozo, M.4
Weiszmann, J.5
Lindberg, R.6
Wang, Y.7
Schwandner, R.8
Li, Y.9
-
92
-
-
84873462479
-
-
International patent application, WO/2006/052566, May 18
-
Leonard, J.N.; Chu, Z.L.; Bruce, M.A.; Boatman, P.D. GPR41 and modulators thereof for the treatment of insulin-related disorders. International patent application, WO/2006/052566, May 18, 2006.
-
(2006)
GPR41 and Modulators Thereof For the Treatment of Insulin-related Disorders
-
-
Leonard, J.N.1
Chu, Z.L.2
Bruce, M.A.3
Boatman, P.D.4
-
93
-
-
73349123182
-
G protein-coupled receptor 43 is essential for neutrophil recruitment during intestinal inflammation
-
Sina, C.; Gavrilova, O.; Förster, M.; Till, A.; Derer, S.; Hildebrand, F.; Raabe, B.; Chalaris, A.; Scheller, J.; Rehmann, A.; Franke, A.; Ott, S.; Häsler, R.; Nikolaus, S.; Fölsch, U.R.; Rose-John, S.; Jiang, H.P.; Li, J.; Schreiber, S.; Rosenstiel, P. G protein-coupled receptor 43 is essential for neutrophil recruitment during intestinal inflammation. J. Immunol., 2009, 183(11), 7514-7522.
-
(2009)
J. Immunol
, vol.183
, Issue.11
, pp. 7514-7522
-
-
Sina, C.1
Gavrilova, O.2
Förster, M.3
Till, A.4
Derer, S.5
Hildebrand, F.6
Raabe, B.7
Chalaris, A.8
Scheller, J.9
Rehmann, A.10
Franke, A.11
Ott, S.12
Häsler, R.13
Nikolaus, S.14
Fölsch, U.R.15
Rose-John, S.16
Jiang, H.P.17
Li, J.18
Schreiber, S.19
Rosenstiel, P.20
more..
-
94
-
-
70350666634
-
Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43
-
Maslowski, K.M.; Vieira, A.T.; Ng, A.; Kranich, J.; Sierro, F.; Yu, D.; Schilter, H.C.; Rolph, M.S.; Mackay, F.; Artis, D.; Xavier, R.J.; Teixeira, M.M.; Mackay, C.R. Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43. Nature, 2009, 461(7268), 1282-1286.
-
(2009)
Nature
, vol.461
, Issue.7268
, pp. 1282-1286
-
-
Maslowski, K.M.1
Vieira, A.T.2
Ng, A.3
Kranich, J.4
Sierro, F.5
Yu, D.6
Schilter, H.C.7
Rolph, M.S.8
Mackay, F.9
Artis, D.10
Xavier, R.J.11
Teixeira, M.M.12
Mackay, C.R.13
-
95
-
-
50449087891
-
Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids
-
Ge, H.; Li, X.; Weiszmann, J.; Wang, P.; Baribault, H.; Chen, J.-L.; Tian, H.; Li, Y. Activation of G protein-coupled receptor 43 in adipocytes leads to inhibition of lipolysis and suppression of plasma free fatty acids. Endocrinology, 2008, 149(9), 4519-4526.
-
(2008)
Endocrinology
, vol.149
, Issue.9
, pp. 4519-4526
-
-
Ge, H.1
Li, X.2
Weiszmann, J.3
Wang, P.4
Baribault, H.5
Chen, J.-L.6
Tian, H.7
Li, Y.8
-
96
-
-
84856509724
-
Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2
-
Tolhurst, G.; Heffron, H.; Lam, YS.; Parker, HE.; Habib, AM.; Diakogiannaki, E.; Cameron, J.; Grosse, J.; Reimann, F.; Gribble, F.M. Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2. Diabetes, 2012, 61(2), 364-371.
-
(2012)
Diabetes
, vol.61
, Issue.2
, pp. 364-371
-
-
Tolhurst, G.1
Heffron, H.2
Lam, Y.S.3
Parker, H.E.4
Habib, A.M.5
Diakogiannaki, E.6
Cameron, J.7
Grosse, J.8
Reimann, F.9
Gribble, F.M.10
-
97
-
-
79958812655
-
SCFAs induce mouse neutrophil chemotaxis through the GPR43 receptor
-
Vinolo, M.A.; Ferguson, G.J.; Kulkarni, S.; Damoulakis, G.; Anderson, K.; Bohlooly, Y.M.; Stephens, L.; Hawkins, P.T.; Curi, R. SCFAs induce mouse neutrophil chemotaxis through the GPR43 receptor. PLoS One, 2011, 6(6), e21205.
-
(2011)
PLoS One
, vol.6
, Issue.6
-
-
Vinolo, M.A.1
Ferguson, G.J.2
Kulkarni, S.3
Damoulakis, G.4
Anderson, K.5
Bohlooly, Y.M.6
Stephens, L.7
Hawkins, P.T.8
Curi, R.9
-
98
-
-
84858285593
-
Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human
-
Ichimura, A.; Hirasawa, A.; Poulain-Godefroy, O.; Bonnefond, A.; Hara, T.; Yengo, L.; Kimura, I.; Leloire, A.; Liu, N.; Iida, K.; Choquet, H.; Besnard, P.; Lecoeur, C.; Vivequin, S.; Ayukawa, K.; Takeuchi, M.; Ozawa, K.; Tauber, M.; Maffeis, C.; Morandi, A.; Buzzetti, R.; Elliott, P.; Pouta, A.; Jarvelin, M.R.; Körner, A.; Kiess, W.; Pigeyre, M.; Caiazzo, R.; Van Hul, W.; Van Gaal, L.; Horber, F.; Balkau, B.; Lévy-Marchal, C.; Rouskas, K.; Kouvatsi, A.; Hebebrand, J.; Hinney, A.; Scherag, A.; Pattou, F.; Meyre, D.; Koshimizu, T.A.; Wolowczuk, I.; Tsujimoto, G.; Froguel, P. Dysfunction of lipid sensor GPR120 leads to obesity in both mouse and human. Nature, 2012, 483(7389), 350-354.
-
(2012)
Nature
, vol.483
, Issue.7389
, pp. 350-354
-
-
Ichimura, A.1
Hirasawa, A.2
Poulain-Godefroy, O.3
Bonnefond, A.4
Hara, T.5
Yengo, L.6
Kimura, I.7
Leloire, A.8
Liu, N.9
Iida, K.10
Choquet, H.11
Besnard, P.12
Lecoeur, C.13
Vivequin, S.14
Ayukawa, K.15
Takeuchi, M.16
Ozawa, K.17
Tauber, M.18
Maffeis, C.19
Morandi, A.20
Buzzetti, R.21
Elliott, P.22
Pouta, A.23
Jarvelin, M.R.24
Körner, A.25
Kiess, W.26
Pigeyre, M.27
Caiazzo, R.28
van Hul, W.29
van Gaal, L.30
Horber, F.31
Balkau, B.32
Lévy-Marchal, C.33
Rouskas, K.34
Kouvatsi, A.35
Hebebrand, J.36
Hinney, A.37
Scherag, A.38
Pattou, F.39
Meyre, D.40
Koshimizu, T.A.41
Wolowczuk, I.42
Tsujimoto, G.43
Froguel, P.44
more..
-
99
-
-
84863516095
-
A systems genetics approach identifies genes and pathways for type 2 diabetes in human islets
-
Taneera, J.; Lang, S.; Sharma, A.; Fadista, J.; Zhou, Y.; Ahlqvist, E.; Jonsson, A.; Lyssenko, V.; Vikman, P.; Hansson, O.; Parikh, H.; Korsgren, O.; Soni, A.; Krus, U.; Zhang, E.; Jing, X.J.; Esguerra, J.L.; Wollheim, C.B.; Salehi, A.; Rosengren, A.; Renström, E.; Groop, L. A systems genetics approach identifies genes and pathways for type 2 diabetes in human islets. Cell Metab., 2012, 16(1), 122-134.
-
(2012)
Cell Metab
, vol.16
, Issue.1
, pp. 122-134
-
-
Taneera, J.1
Lang, S.2
Sharma, A.3
Fadista, J.4
Zhou, Y.5
Ahlqvist, E.6
Jonsson, A.7
Lyssenko, V.8
Vikman, P.9
Hansson, O.10
Parikh, H.11
Korsgren, O.12
Soni, A.13
Krus, U.14
Zhang, E.15
Jing, X.J.16
Esguerra, J.L.17
Wollheim, C.B.18
Salehi, A.19
Rosengren, A.20
Renström, E.21
Groop, L.22
more..
-
100
-
-
57349135245
-
Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists
-
Suzuki, T.; Igari, S.; Hirasawa, A.; Hata, M.; Ishiguro, M.; Fujieda, H.; Itoh, Y.; Hirano, T.; Nakagawa, H.; Ogura, M.; Makishima, M.; Tsujimoto, G.; Miyata, N. Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists. J. Med. Chem., 2008, 51(23), 7640-7644.
-
(2008)
J. Med. Chem
, vol.51
, Issue.23
, pp. 7640-7644
-
-
Suzuki, T.1
Igari, S.2
Hirasawa, A.3
Hata, M.4
Ishiguro, M.5
Fujieda, H.6
Itoh, Y.7
Hirano, T.8
Nakagawa, H.9
Ogura, M.10
Makishima, M.11
Tsujimoto, G.12
Miyata, N.13
-
101
-
-
84861066914
-
Discovery of a potent and selective GPR120 agonist
-
Shimpukade, B.; Hudson, B.D.; Hovgaard, C.K.; Milligan, G.; Ulven, T. Discovery of a potent and selective GPR120 agonist. J. Med. Chem., 2012, 55(9), 4511-4515.
-
(2012)
J. Med. Chem
, vol.55
, Issue.9
, pp. 4511-4515
-
-
Shimpukade, B.1
Hudson, B.D.2
Hovgaard, C.K.3
Milligan, G.4
Ulven, T.5
-
102
-
-
77958142515
-
Structureactivity relationships of GPR120 agonists based on a docking simulation
-
Sun, Q.; Hirasawa, A.; Hara, T.; Kimura, I.; Adachi, T.; Awaji, T.; Ishiguro, M.; Suzuki, T.; Miyata, N.; Tsujimoto, G. Structureactivity relationships of GPR120 agonists based on a docking simulation. Mol. Pharmacol., 2010, 78(5), 804-810.
-
(2010)
Mol. Pharmacol
, vol.78
, Issue.5
, pp. 804-810
-
-
Sun, Q.1
Hirasawa, A.2
Hara, T.3
Kimura, I.4
Adachi, T.5
Awaji, T.6
Ishiguro, M.7
Suzuki, T.8
Miyata, N.9
Tsujimoto, G.10
-
103
-
-
84859949278
-
Differential signaling by splice variants of the human free fatty acid receptor GPR120
-
Watson, S.J.; Brown, A.J.; Holliday, N.D. Differential signaling by splice variants of the human free fatty acid receptor GPR120. Mol. Pharmacol., 2012, 81(5), 631-642.
-
(2012)
Mol. Pharmacol
, vol.81
, Issue.5
, pp. 631-642
-
-
Watson, S.J.1
Brown, A.J.2
Holliday, N.D.3
-
104
-
-
84874364177
-
-
International patent application, WO 2010/104195, September 16
-
Arkawa, K.; Nishimura, T.; Sugimoto, Y.; Takahashi, H. Novel isoindolin-1-one derivative. International patent application, WO 2010/104195, September 16, 2010.
-
(2010)
Novel Isoindolin-1-one Derivative
-
-
Arkawa, K.1
Nishimura, T.2
Sugimoto, Y.3
Takahashi, H.4
-
105
-
-
84874365460
-
-
International patent application, WO 2010/048207, April 29
-
Ma, J.; Novack, A.; Nashashibi, I.; Pham, P.; Rabbat, C.J.; Song, J.; Shi, D.F.; Zhao, Z.; Choi, Y.-J.; Chen, X. Aryl GPR120 receptor agonists and uses therof. International patent application, WO 2010/048207, April 29, 2010.
-
(2010)
Aryl GPR120 Receptor Agonists and Uses Therof
-
-
Ma, J.1
Novack, A.2
Nashashibi, I.3
Pham, P.4
Rabbat, C.J.5
Song, J.6
Shi, D.F.7
Zhao, Z.8
Choi, Y.-J.9
Chen, X.10
-
106
-
-
84864534475
-
-
United States patent application, US 2010/0130559, May 27
-
Hashimoto, N.; Sasaki, Y.; Nakama, C.; Ishikawa, M. Novel phenyl-isoxayol-3-ol derative. United States patent application, US 2010/0130559, May 27, 2010.
-
(2010)
Novel Phenyl-isoxayol-3-ol Derative
-
-
Hashimoto, N.1
Sasaki, Y.2
Nakama, C.3
Ishikawa, M.4
-
107
-
-
68349086914
-
Novel selective ligands for free fatty acid receptors GPR120 and GPR40
-
Hara, T.; Hirasawa, A.; Sun, Q.; Sadakane, K.; Itsubo, C.; Iga, T.; Adachi, T.; Koshimizu, T.; Hashimoto, T.; Asakawa, Y.; Tsujimoto, G. Novel selective ligands for free fatty acid receptors GPR120 and GPR40. Naunyn Schmiedebergs Arch. Pharmacol., 2009, 380(3), 247-255.
-
(2009)
Naunyn Schmiedebergs Arch. Pharmacol
, vol.380
, Issue.3
, pp. 247-255
-
-
Hara, T.1
Hirasawa, A.2
Sun, Q.3
Sadakane, K.4
Itsubo, C.5
Iga, T.6
Adachi, T.7
Koshimizu, T.8
Hashimoto, T.9
Asakawa, Y.10
Tsujimoto, G.11
-
108
-
-
77953287113
-
Agonsim with the omega-3 faty acids α-linolenic acid and docosahexaenoic acid mediates phosphorylation of both the short and long isoforms of the human GPR120 receptor
-
Burns, R.N.; Moniri, N.H. Agonsim with the omega-3 faty acids α-linolenic acid and docosahexaenoic acid mediates phosphorylation of both the short and long isoforms of the human GPR120 receptor. Biochem. Biophys. Res. Commun., 2010, 396(4), 1030-1035.
-
(2010)
Biochem. Biophys. Res. Commun
, vol.396
, Issue.4
, pp. 1030-1035
-
-
Burns, R.N.1
Moniri, N.H.2
-
109
-
-
0034978118
-
Cloning and expression analysis of a novel G-protein-coupled receptor selectively expressed on granulocytes
-
Yousefi, S.; Cooper, P.R.; Potter, S.L.; Mueck, B.; Jarai, G. Cloning and expression analysis of a novel G-protein-coupled receptor selectively expressed on granulocytes. J. Leukoc. Biol., 2001, 69(6), 1045-1052.
-
(2001)
J. Leukoc. Biol
, vol.69
, Issue.6
, pp. 1045-1052
-
-
Yousefi, S.1
Cooper, P.R.2
Potter, S.L.3
Mueck, B.4
Jarai, G.5
-
110
-
-
34249062904
-
G protein-coupled receptor 84, a microglia-associated protein expressed in neuroinflammatory conditions
-
Bouchard C.; Pagé, J.; Bédard, A.; Tremblay, P.; Vallières, L. G protein-coupled receptor 84, a microglia-associated protein expressed in neuroinflammatory conditions. Glia, 2007, 55, 790-800.
-
(2007)
Glia
, vol.55
, pp. 790-800
-
-
Bouchard, C.1
Pagé, J.2
Bédard, A.3
Tremblay, P.4
Vallières, L.5
-
111
-
-
84857051975
-
Inflammatory changes in adipose tissue enhance expression of GPR84; a medium-chain fatty acid receptor: TNFα enhances GPR84 expression in adipocytes
-
Nagasaki, H.; Kondo, T.; Fuchigami, M.; Hashimoto, H.; Sugimura, Y.; Ozaki, N.; Arima, H.; Ota, A.; Oiso, Y.; Hamada, Y. Inflammatory changes in adipose tissue enhance expression of GPR84; a medium-chain fatty acid receptor: TNFα enhances GPR84 expression in adipocytes. FEBS Lett., 2012, 586(4), 368-372.
-
(2012)
FEBS Lett
, vol.586
, Issue.4
, pp. 368-372
-
-
Nagasaki, H.1
Kondo, T.2
Fuchigami, M.3
Hashimoto, H.4
Sugimura, Y.5
Ozaki, N.6
Arima, H.7
Ota, A.8
Oiso, Y.9
Hamada, Y.10
-
112
-
-
0242321259
-
Identification of surrogate ligands for orphan G protein-coupled receptors
-
Takeda, S.; Yamamoto, A.; Okada, T.; Matsumura, E.; Nose, E.; Kogure, K.; Kojima, S.; Haga, T. Identification of surrogate ligands for orphan G protein-coupled receptors. Life Sci., 2003, 74(2-3), 367-377.
-
(2003)
Life Sci
, vol.74
, Issue.2-3
, pp. 367-377
-
-
Takeda, S.1
Yamamoto, A.2
Okada, T.3
Matsumura, E.4
Nose, E.5
Kogure, K.6
Kojima, S.7
Haga, T.8
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