-
1
-
-
0028229508
-
Insulin resistance or insulin deficiency. Which is the primary cause of NIDDM?
-
Taylor, S. I.; Accili, D.; Imai, Y. Insulin resistance or insulin deficiency. Which is the primary cause of NIDDM? Diabetes 1994, 43, 735-740
-
(1994)
Diabetes
, vol.43
, pp. 735-740
-
-
Taylor, S.I.1
Accili, D.2
Imai, Y.3
-
2
-
-
0027458051
-
Insulin resistance and insulin deficiency in the pathogenesis of Type 2 (non-insulin-dependent) diabetes mellitus: Errors of metabolism or of methods?
-
DOI 10.1007/BF00400814
-
Groop, L. C.; Widen, E.; Ferrannini, E. Insulin resistance and insulin deficiency in the pathogenesis of type 2 (non-insulin-dependent) diabetes mellitus: errors of metabolism or of methods? Diabetologia 1993, 36, 1326-1331 (Pubitemid 23353035)
-
(1993)
Diabetologia
, vol.36
, Issue.12
, pp. 1326-1331
-
-
Groop, L.C.1
Widen, E.2
Ferrannini, E.3
-
3
-
-
0012873550
-
Pathogenesis of type 2 diabetes: The relative contribution of insulin resistance and impaired insulin secretion
-
Groop, L. Pathogenesis of type 2 diabetes: the relative contribution of insulin resistance and impaired insulin secretion Int. J. Clin. Pract., Suppl. 2000, 113, 3-13
-
(2000)
Int. J. Clin. Pract., Suppl.
, vol.113
, pp. 3-13
-
-
Groop, L.1
-
4
-
-
0032449219
-
The genetic basis of type 2 diabetes mellitus: Impaired insulin secretion versus impaired insulin sensitivity
-
Gerich, J. The genetic basis of type 2 diabetes mellitus: impaired insulin secretion versus impaired insulin sensitivity Endocr. Rev. 1998, 19, 491-503 (Pubitemid 29116017)
-
(1998)
Endocrine Reviews
, vol.19
, Issue.4
, pp. 491-503
-
-
Gerich, J.E.1
-
5
-
-
0030971593
-
Effect of a new hypoglycemic agent, A-4166 [(-)-N-(trans-4-isopropyl- cyclohexanecarbonyl)-D-phenylalanine], on postprandial blood glucose excursion: Comparison with voglibose and glibenclamide
-
Ikenoue, T.; Okazaki, K.; Fujitani, S.; Tsuchiya, Y.; Akiyoshi, M.; Maki, T.; Kondo, N. Effect of a new hypoglycemic agent, A-4166 [(-)- N -(trans -4-isopropylcyclohexanecarbonyl)- d -phenylalanine], on postprandial blood glucose excursion: comparison with voglibose and glibenblamide Biol. Pharm. Bull. 1997, 20, 354-359 (Pubitemid 27212992)
-
(1997)
Biological and Pharmaceutical Bulletin
, vol.20
, Issue.4
, pp. 354-359
-
-
Ikenoue, T.1
Okazaki, K.2
Fujitani, S.3
Tsuchiya, Y.4
Akiyoshi, M.5
Maki, T.6
Kondo, N.7
-
6
-
-
3142728651
-
The role of sulphonylureas in the management of type 2 diabetes mellitus
-
DOI 10.2165/00003495-200464120-00006
-
Rendell, M. The role of sulphonylureas in the management of type 2 diabetes mellitus Drugs 2004, 64, 1339-1358 (Pubitemid 38916346)
-
(2004)
Drugs
, vol.64
, Issue.12
, pp. 1339-1358
-
-
Rendell, M.1
-
7
-
-
0020578096
-
Glibenclamide-associated hypoglycaemia: A report on 57 cases
-
Asplund, K.; Wiholm, B. E.; Lithner, F. Glibenclamide-associated hypoglycaemia: a report on 57 cases Diabetologia 1983, 24, 412-417
-
(1983)
Diabetologia
, vol.24
, pp. 412-417
-
-
Asplund, K.1
Wiholm, B.E.2
Lithner, F.3
-
8
-
-
0023935536
-
Sulphonylureas and hypoglycaemia
-
Ferner, R. E.; Neil, H. A. Sulphonylureas and hypoglycaemia Br. Med. J. (Clin. Res. Ed.) 1988, 296, 949-950 (Pubitemid 18093424)
-
(1988)
British Medical Journal
, vol.296
, Issue.6627
, pp. 949-950
-
-
Ferner, R.E.1
Neil, H.A.W.2
-
9
-
-
12244287074
-
Sulfonylurea induced β-cell apoptosis in cultured human islets
-
DOI 10.1210/jc.2004-0699
-
Maedler, K.; Carr, R. D.; Bosco, D.; Zuellig, R. A.; Berney, T.; Donath, M. Y. Sulfonylurea induced beta-cell apoptosis in cultured human islets J. Clin. Endocrinol. Metab. 2005, 90, 501-506 (Pubitemid 40116700)
-
(2005)
Journal of Clinical Endocrinology and Metabolism
, vol.90
, Issue.1
, pp. 501-506
-
-
Maedler, K.1
Carr, R.D.2
Bosco, D.3
Zuellig, R.A.4
Berney, T.5
Donath, M.Y.6
-
10
-
-
11844298435
-
Effects of prolonged in vitro exposure to sulphonylureas on the function and survival of human islets
-
DOI 10.1016/j.jdiacomp.2004.05.001, PII S1056872704000546
-
Del Guerra, S.; Marselli, L.; Lupi, R.; Boggi, U.; Mosca, F.; Benzi, L.; Del Prato, S.; Marchetti, P. Effects of prolonged in vitro exposure to sulphonylureas on the function and survival of human islets J. Diabetes Complications 2005, 19, 60-64 (Pubitemid 40092372)
-
(2005)
Journal of Diabetes and its Complications
, vol.19
, Issue.1
, pp. 60-64
-
-
Del Guerra, S.1
Marselli, L.2
Lupi, R.3
Boggi, U.4
Mosca, F.5
Benzi, L.6
Del Prato, S.7
Marchetti, P.8
-
11
-
-
33846006173
-
The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes
-
DOI 10.1016/S0140-6736(06)69705-5, PII S0140673606697055
-
Drucker, D. J.; Nauck, M. A. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes Lancet 2006, 368, 1696-1705 (Pubitemid 46048557)
-
(2006)
Lancet
, vol.368
, Issue.9548
, pp. 1696-1705
-
-
Drucker, D.J.1
Nauck, M.A.2
-
12
-
-
0028221978
-
Mechanisms of the stimulation of insulin release by saturated fatty acids: A study of palmitate effects in mouse β-cells
-
Warnotte, C.; Gilon, P.; Nenquin, M.; Henquin, J. C. Mechanisms of the stimulation of insulin release by saturated fatty acids: a study of palmitate effects in mouse β-cells Diabetes 1994, 43, 703-711 (Pubitemid 24138785)
-
(1994)
Diabetes
, vol.43
, Issue.5
, pp. 703-711
-
-
Warnotte, C.1
Gilon, P.2
Nenquin, M.3
Henquin, J.-C.4
-
13
-
-
0036896505
-
Malonyl-CoA signaling, lipid partitioning, and glucolipotoxicity: Role in beta-cell adaptation and failure in the etiology of diabetes
-
Prentki, M; Joly, E.; El-Assaad, W.; Roduit, R. Malonyl-CoA signaling, lipid partitioning, and glucolipotoxicity: role in beta-cell adaptation and failure in the etiology of diabetes Diabetes 2002, 51 (Suppl 3) S405-S413
-
(2002)
Diabetes
, vol.51
, Issue.SUPPL. 3
-
-
Prentki, M.1
Joly, E.2
El-Assaad, W.3
Roduit, R.4
-
14
-
-
12144291143
-
A Role for the Malonyl-CoA/Long-Chain Acyl-CoA Pathway of Lipid Signaling in the Regulation of Insulin Secretion in Response to Both Fuel and Nonfuel Stimuli
-
DOI 10.2337/diabetes.53.4.1007
-
Roduit, R.; Nolan, C.; Alarcon, C.; Moore, P.; Barbeau, A.; Delghingaro-Augusto, V.; Przybykowski, E.; Morin, J.; Massé, F.; Massie, B.; Ruderman, N.; Rhodes, C.; Poitout, V.; Prentki, M. A role for the malonyl-CoA/long-chain acyl-CoA pathway of lipid signaling in the regulation of insulin secretion in response to both fuel and nonfuel stimuli Diabetes 2004, 53, 1007-1019 (Pubitemid 38436613)
-
(2004)
Diabetes
, vol.53
, Issue.4
, pp. 1007-1019
-
-
Roduit, R.1
Nolan, C.2
Alarcon, C.3
Moore, P.4
Barbeau, A.5
Delghingaro-Augusto, V.6
Przybykowski, E.7
Morin, J.8
Masse, F.9
Massie, B.10
Ruderman, N.11
Rhodes, C.12
Poitout, V.13
Prentki, M.14
-
15
-
-
0027400494
-
Amplification of insulin secretion by lipid messengers
-
Turk, J.; Gross, R. W.; Ramanadham, S. Amplification of insulin secretion by lipid messengers Diabetes 1993, 42, 367-374 (Pubitemid 23066511)
-
(1993)
Diabetes
, vol.42
, Issue.3
, pp. 367-374
-
-
Turk, J.1
Gross, R.W.2
Ramanadham, S.3
-
16
-
-
0037434991
-
Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40
-
DOI 10.1038/nature01478
-
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, 173-176 (Pubitemid 36362750)
-
(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..
-
17
-
-
0037838892
-
The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
-
DOI 10.1074/jbc.M211495200
-
Briscoe, C. P.; Tadayyon, M.; Andrews, J. L.; Benson, W. G.; Chambers, J. K.; Eilert, M. M.; Eillis, 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 (Pubitemid 36792687)
-
(2003)
Journal of Biological Chemistry
, 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.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
Szekeres, P.G.16
Tan, K.B.17
Way, J.M.18
Ignar, D.M.19
Wilson, S.20
Muir, A.I.21
more..
-
18
-
-
0037423719
-
A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs
-
DOI 10.1016/S0006-291X(02)03064-4
-
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, 406-410 (Pubitemid 36279253)
-
(2003)
Biochemical and Biophysical Research Communications
, vol.301
, Issue.2
, pp. 406-410
-
-
Kotarsky, K.1
Nilsson, N.E.2
Flodgren, E.3
Owman, C.4
Olde, B.5
-
19
-
-
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, 405-417
-
(2008)
Pharmacol. Rev.
, vol.60
, pp. 405-417
-
-
Stoddart, L.A.1
Smith, N.J.2
Milligan, G.3
-
20
-
-
0030748260
-
Signal transduction mechanisms in nutrient-induced insulin secretion
-
Prentki, M.; Tornheim, K.; Corkey, B. E. Signal transduction mechanisms in nutrient-induced insulin secretion Diabetologia 1997, 40, S32-S41
-
(1997)
Diabetologia
, vol.40
-
-
Prentki, M.1
Tornheim, K.2
Corkey, B.E.3
-
23
-
-
25144433441
-
Role of GPR40 in fatty acid action on the β cell line INS-1E
-
DOI 10.1016/j.bbrc.2005.07.042, PII S0006291X05014774
-
Shapiro, H.; Shachar, S.; Sekler, I.; Hershfinkel, M.; Walker, M. D. Role of GPR40 in fatty acid action on the β cell line INS-1E Biochem. Biophys. Res. Commun. 2005, 335, 97-104 (Pubitemid 41350767)
-
(2005)
Biochemical and Biophysical Research Communications
, vol.335
, Issue.1
, pp. 97-104
-
-
Shapiro, H.1
Shachar, S.2
Sekler, I.3
Hershfinkel, M.4
Walker, M.D.5
-
24
-
-
33751520308
-
Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from β-cells through activation of GPR40
-
DOI 10.1016/j.mce.2006.09.013, PII S0303720706004758
-
Schnell, S.; Schaefer, M.; Schofl, C. Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40 Mol. Cell. Endocrinol. 2007, 263, 173-180 (Pubitemid 44834553)
-
(2007)
Molecular and Cellular Endocrinology
, vol.263
, Issue.1-2
, pp. 173-180
-
-
Schnell, S.1
Schaefer, M.2
Schofl, C.3
-
25
-
-
65549114432
-
Overexpression of GPR40 in pancreatic β-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice
-
Nagasumi, K.; Esaki, R.; Iwachidow, K.; Yasuhara, Y.; Ogi, K.; Tanaka, H.; Nakata, M.; Yano, T.; Shimakawa, K.; Taketomi, S.; Takeuchi, K.; Odaka, H.; Kaisho, Y. Overexpression of GPR40 in pancreatic β-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice Diabetes 2009, 58, 1067-1076
-
(2009)
Diabetes
, vol.58
, pp. 1067-1076
-
-
Nagasumi, K.1
Esaki, R.2
Iwachidow, K.3
Yasuhara, Y.4
Ogi, K.5
Tanaka, H.6
Nakata, M.7
Yano, T.8
Shimakawa, K.9
Taketomi, S.10
Takeuchi, K.11
Odaka, H.12
Kaisho, Y.13
-
26
-
-
33745607930
-
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: Identification of agonist and antagonist small molecules
-
DOI 10.1038/sj.bjp.0706770, PII 0706770
-
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 (Pubitemid 43993052)
-
(2006)
British Journal of Pharmacology
, 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
-
27
-
-
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, 2211-2219
-
(2008)
Diabetes
, vol.57
, 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
-
28
-
-
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
-
Tsujihata, 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, 228-237
-
(2011)
J. Pharmacol. Exp. Ther.
, vol.339
, pp. 228-237
-
-
Tsujihata, Y.1
Ito, R.2
Suzuki, M.3
Harada, A.4
Negoro, N.5
Yasuma, T.6
Momose, Y.7
Takeuchi, K.8
-
29
-
-
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 ACS Med. Chem. Lett. 2010, 1, 290-294
-
(2010)
ACS 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..
-
30
-
-
79952261037
-
Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists
-
Sasaki, S.; Kitamura, S.; Negoro, N.; Suzuki, M.; Tsujihata, Y.; Suzuki, N.; Santou, T.; Kanzaki, N.; Harada, M.; Tanaka, Y.; Kobayashi, M.; Tada, N.; Funami, M.; Tanaka, T.; Yamamoto, Y.; Fukatsu, K.; Yasuma, T.; Momose, Y. Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists J. Med. Chem. 2011, 54, 1365-1378
-
(2011)
J. Med. Chem.
, vol.54
, pp. 1365-1378
-
-
Sasaki, S.1
Kitamura, S.2
Negoro, N.3
Suzuki, M.4
Tsujihata, Y.5
Suzuki, N.6
Santou, T.7
Kanzaki, N.8
Harada, M.9
Tanaka, Y.10
Kobayashi, M.11
Tada, N.12
Funami, M.13
Tanaka, T.14
Yamamoto, Y.15
Fukatsu, K.16
Yasuma, T.17
Momose, Y.18
-
31
-
-
33644938799
-
Comparison of in vitro assays of cellular toxicity in the human hepatic cell line HepG2
-
Miret, M.; de Groene, E. M.; Klaffke, W. Comparison of in vitro assays of cellular toxicity in the human hepatic cell line HepG2 J. Biomol. Screening 2006, 11, 184-193
-
(2006)
J. Biomol. Screening
, vol.11
, pp. 184-193
-
-
Miret, M.1
De Groene, E.M.2
Klaffke, W.3
-
32
-
-
0033639131
-
A strategy for primary high throughput cytotoxicity screening in pharmaceutical toxicology
-
Bugelski, P. J.; Atif, U.; Molton, S.; Toeg, I.; Lord, P. G.; Morgan, D. G. A strategy for primary high throughput cytotoxicity screening in pharmaceutical toxicology Pharm. Res. 2000, 17, 1265-1272
-
(2000)
Pharm. Res.
, vol.17
, pp. 1265-1272
-
-
Bugelski, P.J.1
Atif, U.2
Molton, S.3
Toeg, I.4
Lord, P.G.5
Morgan, D.G.6
-
33
-
-
0032839104
-
Overview of the final MEIC results: II. The in vitro-in vivo evaluation, including the selection of a practical battery of cell tests for prediction of acute lethal blood concentrations in humans
-
DOI 10.1016/S0887-2333(99)00061-2, PII S0887233399000612
-
Ekwall, B. Overview of the final MEIC results: II. The in vitro-in vivo evaluation, including the selection of a practical battery of cell tests for prediction of acute lethal blood concentrations in humans Toxicol. in Vitro 1999, 13, 665-673 (Pubitemid 29354194)
-
(1999)
Toxicology in Vitro
, vol.13
, Issue.4-5
, pp. 665-673
-
-
Ekwall, B.1
-
34
-
-
24644511815
-
Research perspectives for pre-screening alternatives to animal experimentation: On the relevance of cytotoxicity measurements, barrier passage determinations and high throughput screening in vitro to select potentially hazardous compounds in large sets of chemicals
-
Walum, E.; Hedander, J.; Garberg, P. Research perspectives for pre-screening alternatives to animal experimentation: on the relevance of cytotoxicity measurements, barrier passage determinations and high throughput screening in vitro to select potentially hazardous compounds in large sets of chemicals Toxicol. Appl. Pharmacol. 2005, 207, S393-S397
-
(2005)
Toxicol. Appl. Pharmacol.
, vol.207
-
-
Walum, E.1
Hedander, J.2
Garberg, P.3
-
35
-
-
67649331670
-
Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): An emerging target for type 2 diabetes
-
Bharate, S. B.; Nemmani, K. V.; Vishwakarma, R. A. Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1): an emerging target for type 2 diabetes Expert Opin. Ther. Pat. 2009, 19, 237-264
-
(2009)
Expert Opin. Ther. Pat.
, vol.19
, pp. 237-264
-
-
Bharate, S.B.1
Nemmani, K.V.2
Vishwakarma, R.A.3
-
36
-
-
33144463383
-
Synthesis and activity of small molecule GPR40 agonists
-
DOI 10.1016/j.bmcl.2006.01.007, PII S0960894X06000242
-
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 (Pubitemid 43267362)
-
(2006)
Bioorganic and Medicinal Chemistry Letters
, vol.16
, Issue.7
, pp. 1840-1845
-
-
Garrido, D.M.1
Corbett, D.F.2
Dwornik, K.A.3
Goetz, A.S.4
Littleton, T.R.5
McKeown, S.C.6
Mills, W.Y.7
Smalley Jr., T.L.8
Briscoe, C.P.9
Peat, A.J.10
-
37
-
-
74049162863
-
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists
-
Zhou, C.; Tang, C.; Chang, E.; Ge, M.; Lin, S.; Cline, E.; Tan, C. P.; Feng, Y.; Zhou, Y. P.; Eiermann, G. J.; Petrov, A.; Salituro, G.; Meinke, P.; Mosley, R.; Akiyama, T. E.; Einstein, M.; Kumar, S.; Berger, J.; Howard, A. D.; Thornberry, N.; Mills, S. G.; Yang, L. Discovery of 5-aryloxy-2,4- thiazolidinediones as potent GPR40 agonists Bioorg. Med. Chem. Lett. 2010, 20, 1298-1301
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1298-1301
-
-
Zhou, C.1
Tang, C.2
Chang, E.3
Ge, M.4
Lin, S.5
Cline, E.6
Tan, C.P.7
Feng, Y.8
Zhou, Y.P.9
Eiermann, G.J.10
Petrov, A.11
Salituro, G.12
Meinke, P.13
Mosley, R.14
Akiyama, T.E.15
Einstein, M.16
Kumar, S.17
Berger, J.18
Howard, A.D.19
Thornberry, N.20
Mills, S.G.21
Yang, L.22
more..
-
38
-
-
34250879091
-
Synthesis and biological evaluation of 3-aryl-3-(4-phenoxy)-propionic acid as a novel series of G protein-coupled receptor 40 agonists
-
DOI 10.1021/jm070130j
-
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 (Pubitemid 46980852)
-
(2007)
Journal of Medicinal Chemistry
, vol.50
, Issue.12
, pp. 2807-2817
-
-
Song, F.1
Lu, S.2
Gunnet, J.3
Xu, J.Z.4
Wines, P.5
Proost, J.6
Liang, Y.7
Baumann, C.8
Lenhard, J.9
Murray, W.V.10
Demarest, K.T.11
Kuo, G.-H.12
-
39
-
-
79251476856
-
Development of a suitable salt form for a GPR40 receptor agonist
-
Morrison, H.; Jona, J.; Walker, S. D.; Woo, J. C. S.; Li, L.; Fang, J. Development of a suitable salt form for a GPR40 receptor agonist Org. Process Res. Dev. 2011, 15, 104-111
-
(2011)
Org. Process Res. Dev.
, vol.15
, pp. 104-111
-
-
Morrison, H.1
Jona, J.2
Walker, S.D.3
Woo, J.C.S.4
Li, L.5
Fang, J.6
-
40
-
-
77958099021
-
Structure-activity study of dihydrocinnamic acids and discovery of the potent FFA1 (GPR40) agonist TUG-469
-
Christiansen, E.; Due-Hansen, M. E.; Urban, C.; Merten, N.; Pfleiderer, M.; Karlsen, K. K.; Rasmussen, S. S.; Steensgaard, M.; Hamacher, A.; Schmidt, J.; Drewke, C.; Petersen, R. K.; Kristiansen, K.; Ullrich, S.; Kostenis, E.; Kassack, M. U.; Ulven, T. Structure-activity study of dihydrocinnamic acids and discovery of the potent FFA1 (GPR40) agonist TUG-469 ACS Med. Chem. Lett. 2010, 1, 345-349
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, pp. 345-349
-
-
Christiansen, E.1
Due-Hansen, M.E.2
Urban, C.3
Merten, N.4
Pfleiderer, M.5
Karlsen, K.K.6
Rasmussen, S.S.7
Steensgaard, M.8
Hamacher, A.9
Schmidt, J.10
Drewke, C.11
Petersen, R.K.12
Kristiansen, K.13
Ullrich, S.14
Kostenis, E.15
Kassack, M.U.16
Ulven, T.17
-
41
-
-
56749163623
-
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
-
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 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes J. Med. Chem. 2008, 51, 7061-7064
-
(2008)
J. Med. Chem.
, vol.51
, 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
-
42
-
-
80053910894
-
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties
-
Christiansen, E.; Urban, C.; Grundmann, M.; Deu-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 receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties J. Med. Chem. 2011, 54, 6691-6703
-
(2011)
J. Med. Chem.
, vol.54
, pp. 6691-6703
-
-
Christiansen, E.1
Urban, C.2
Grundmann, M.3
Deu-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
-
43
-
-
84855673463
-
AMG 837: A potent, orally bioavailable GPR40 agonist
-
Houze, J. B.; Zhu, L.; Sun, Y.; Akerman, M.; Qiu, W.; Zhang, A. J.; Sharma, R.; Schmitt, M.; Wang, Y.; Liu, J.; Liu, J.; Medina, J. C.; Reagan, J. D.; Luo, J.; Tonn, G.; Zhang, J.; Lu, J. Y-L.; Chen, M.; Lopez, E.; Nguyen, K.; Yang, L.; Tang, L.; Tian, H.; Shuttleworth, S. J.; Lin, D. C. AMG 837: A potent, orally bioavailable GPR40 agonist Bioorg. Med. Chem. Lett. 2012, 22, 1267-1270
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 1267-1270
-
-
Houze, J.B.1
Zhu, L.2
Sun, Y.3
Akerman, M.4
Qiu, W.5
Zhang, A.J.6
Sharma, R.7
Schmitt, M.8
Wang, Y.9
Liu, J.10
Liu, J.11
Medina, J.C.12
Reagan, J.D.13
Luo, J.14
Tonn, G.15
Zhang, J.16
Lu, J.Y.-L.17
Chen, M.18
Lopez, E.19
Nguyen, K.20
Yang, L.21
Tang, L.22
Tian, H.23
Shuttleworth, S.J.24
Lin, D.C.25
more..
-
44
-
-
49849094738
-
Physiochemical drug properties associated with in vivo toxicological outcomes
-
Hughes, J. D.; Blagg, J.; Price, D. A.; Bailey, S.; Decrescenzo, G. A.; Devraj, R. V.; Ellsworth, E.; Fobian, Y. M.; Gibbs, M. E.; Gilles, R. W.; Greene, N.; Huang, E.; Krieger-Burke, T.; Loesel, J.; Wager, T.; Whiteley, L.; Zhang, Y. Physiochemical drug properties associated with in vivo toxicological outcomes Bioorg. Med. Chem. Lett. 2008, 18, 4872-4875
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4872-4875
-
-
Hughes, J.D.1
Blagg, J.2
Price, D.A.3
Bailey, S.4
Decrescenzo, G.A.5
Devraj, R.V.6
Ellsworth, E.7
Fobian, Y.M.8
Gibbs, M.E.9
Gilles, R.W.10
Greene, N.11
Huang, E.12
Krieger-Burke, T.13
Loesel, J.14
Wager, T.15
Whiteley, L.16
Zhang, Y.17
-
45
-
-
35748934487
-
The influence of drug-like concepts on decision-making in medicinal chemistry
-
DOI 10.1038/nrd2445, PII NRD2445
-
Leeson, P. D.; Springthorpe, B. The influence of drug-like concepts on decision-making in medicinal chemistry Nature Rev. Drug Discovery 2007, 6, 881-890 (Pubitemid 350042396)
-
(2007)
Nature Reviews Drug Discovery
, vol.6
, Issue.11
, pp. 881-890
-
-
Leeson, P.D.1
Springthorpe, B.2
-
46
-
-
77749315417
-
Lipophilicity in drug discovery
-
Waring, M. J. Lipophilicity in drug discovery Expert Opin. Drug Discovery 2010, 5, 235-248
-
(2010)
Expert Opin. Drug Discovery
, vol.5
, pp. 235-248
-
-
Waring, M.J.1
-
47
-
-
0038363378
-
The orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids
-
DOI 10.1074/jbc.M211609200
-
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, 11312-11319 (Pubitemid 36792688)
-
(2003)
Journal of Biological Chemistry
, 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..
-
48
-
-
13444263540
-
Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120
-
DOI 10.1038/nm1168
-
Hirasawa, A.; Tsumaya, K.; Awaji, T.; Katsuma, S.; Adachi, T.; Yamada, M.; Sugimoto, Y.; Miyazaki, S.; Tsujimoto, G. Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120 Nature Med. 2005, 11, 90-94 (Pubitemid 40215843)
-
(2005)
Nature Medicine
, vol.11
, Issue.1
, pp. 90-94
-
-
Hirasawa, A.1
Tsumaya, K.2
Awaji, T.3
Katsuma, S.4
Adachi, T.5
Yamada, M.6
Sugimoto, Y.7
Miyazaki, S.8
Tsujimoto, G.9
-
49
-
-
53549127020
-
Free fatty acid receptors and drug discovery
-
Hirasawa, A.; Hara, T.; Katsuma, S.; Adachi, T.; Tsujimoto, G. Free fatty acid receptors and drug discovery Biol. Pharm. Bull. 2008, 31, 1847-1851
-
(2008)
Biol. Pharm. Bull.
, vol.31
, pp. 1847-1851
-
-
Hirasawa, A.1
Hara, T.2
Katsuma, S.3
Adachi, T.4
Tsujimoto, G.5
-
50
-
-
57049170465
-
Fatty acid binding receptors and their physiological role in type 2 diabetes
-
Swaminath, G. Fatty acid binding receptors and their physiological role in type 2 diabetes Arch. Pharm. (Weinheim, Ger.) 2008, 341, 753-761
-
(2008)
Arch. Pharm. (Weinheim, Ger.)
, vol.341
, pp. 753-761
-
-
Swaminath, G.1
-
51
-
-
70350309324
-
Lipid receptors and islet function: Therapeutic implications?
-
Kebede, M. A.; Alquier, T.; Latour, M. G.; Poitout, V. Lipid receptors and islet function: therapeutic implications? Diabetes, Obes. Metab. 2009, 11, 10-20
-
(2009)
Diabetes, Obes. Metab.
, vol.11
, pp. 10-20
-
-
Kebede, M.A.1
Alquier, T.2
Latour, M.G.3
Poitout, V.4
-
52
-
-
0036183630
-
The mechanisms of action of PPARs
-
DOI 10.1146/annurev.med.53.082901.104018
-
Berger, J.; Moller, D. E. The mechanisms of action of PPARs Annu. Rev. Med. 2002, 53, 409-435 (Pubitemid 34177889)
-
(2002)
Annual Review of Medicine
, vol.53
, pp. 409-435
-
-
Berger, J.1
Moller, D.E.2
-
53
-
-
0037643536
-
Effects of free fatty acids (FFA) on glucose metabolism: Significance for insulin resistance and type 2 diabetes
-
DOI 10.1055/s-2003-39781
-
Boden, G. Effects of free fatty acids (FFA) on glucose metabolism: significance for insulin resistance and type 2 diabetes Exp. Clin. Endocrinol. Diabetes 2003, 111, 121-124 (Pubitemid 36682048)
-
(2003)
Experimental and Clinical Endocrinology and Diabetes
, vol.111
, Issue.3
, pp. 121-124
-
-
Boden, G.1
-
54
-
-
0344406146
-
Mechanisms of the free fatty acid-induced increase in hepatic glucose production
-
Lam, T. K.; Carpentier, A.; Lewis, G. F.; van de Werve, G.; Fantus, I. G.; Giacca, A. Mechanisms of the free fatty acid-induced increase in hepatic glucose production Am. J. Physiol. Endocrinol. Metab. 2003, 284, E863-E873
-
(2003)
Am. J. Physiol. Endocrinol. Metab.
, vol.284
-
-
Lam, T.K.1
Carpentier, A.2
Lewis, G.F.3
Van De Werve, G.4
Fantus, I.G.5
Giacca, A.6
-
55
-
-
0025030095
-
Hydrophobicity parameters determined by reversed-phase liquid chromatography. I. Relationship between capacity factors and octanol-water partition coefficients for monosubstituted pyrazines and the related pyridines
-
Yamagami, C.; Ogura, T.; Takao, N. Hydrophobicity parameters determined by reversed-phase liquid chromatography I. Relationship between capacity factors and octanol-water partition coefficients for monosubstituted pyrazines and the related pyridines J. Chromatogr. 1990, 514, 123-136 (Pubitemid 20256620)
-
(1990)
Journal of Chromatography
, vol.514
, Issue.2
, pp. 123-136
-
-
Yamagami, C.1
Ogura, T.2
Takao, N.3
-
56
-
-
0019743219
-
A new genetically obese-hyperglycemic rat (Wistar fatty)
-
Ikeda, H.; Shino, A.; Matsuo, T.; Iwatsuka, H.; Suzuoki, Z. A new genetically obese-hyperglycemic rat (Wistar fatty) Diabetes 1981, 30, 1045-1050
-
(1981)
Diabetes
, vol.30
, pp. 1045-1050
-
-
Ikeda, H.1
Shino, A.2
Matsuo, T.3
Iwatsuka, H.4
Suzuoki, Z.5
-
57
-
-
6344248639
-
Structure of bovine rhodopsin in a trigonal crystal form
-
DOI 10.1016/j.jmb.2004.08.090, PII S0022283604010903
-
Li, J.; Edwards, P. C.; Burghammer, M.; Villa, C.; Schertler, G. F. Structure of bovine rhodopsin in a trigonal crystal form J. Mol. Biol. 2004, 343, 1409-1438 (Pubitemid 39387834)
-
(2004)
Journal of Molecular Biology
, vol.343
, Issue.5
, pp. 1409-1438
-
-
Li, J.1
Edwards, P.C.2
Burghammer, M.3
Villa, C.4
Schertler, G.F.X.5
-
58
-
-
36448991500
-
Clustal W and Clustal X version 2.0
-
DOI 10.1093/bioinformatics/btm404
-
Larkin, M. A.; Blackshields, G.; Brown, N. P.; Chenna, R.; McGettigan, P. A.; McWilliam, H.; Valentin, F.; Wallace, I. M.; Wilm, A.; Lopez, R.; Thompson, J. D.; Gibson, T. J.; Higgins, D. G. Clustal W and clustal X version 2.0 Bioinformatics 2007, 23, 2947-2948 (Pubitemid 350162903)
-
(2007)
Bioinformatics
, vol.23
, Issue.21
, pp. 2947-2948
-
-
Larkin, M.A.1
Blackshields, G.2
Brown, N.P.3
Chenna, R.4
Mcgettigan, P.A.5
McWilliam, H.6
Valentin, F.7
Wallace, I.M.8
Wilm, A.9
Lopez, R.10
Thompson, J.D.11
Gibson, T.J.12
Higgins, D.G.13
-
59
-
-
79751531734
-
-
Chemical Computing Group Inc. 1010 Sherbrooke St. W, Suite 910 Montreal, Quebec, Canada H3A 2R7.
-
MOE, version 2008.10; Chemical Computing Group Inc.: 1010 Sherbrooke St. W, Suite 910 Montreal, Quebec, Canada H3A 2R7, 2008; http://www.chemcomp.com.
-
(2008)
MOE, Version 2008.10
-
-
-
60
-
-
84860287448
-
-
CCDC, Business & Administration, Cambridge Crystallographic Data Centre: 12 Union Road, Cambridge CB2 1EZ, U.K.
-
GOLD, version 4.1; CCDC, Business & Administration, Cambridge Crystallographic Data Centre: 12 Union Road, Cambridge CB2 1EZ, U.K., 2010; http://www.ccdc.cam.ac.uk.
-
(2010)
GOLD, Version 4.1
-
-
|