-
1
-
-
67349139275
-
Assessing the potential of glucokinase activators in diabetes therapy
-
Matschinsky, F. M. Assessing the potential of glucokinase activators in diabetes therapy. Nat. Rev. Drug Discov. 2009, 8, 399-416.
-
(2009)
Nat. Rev. Drug Discov.
, vol.8
, pp. 399-416
-
-
Matschinsky, F.M.1
-
2
-
-
48049120189
-
Glucokinase activators as new type 2 diabetes therapeutic agents
-
Sarabu, R.; Berthel, S. J.; Kester, R. F. K.; Tilley, J. W. T. Glucokinase activators as new type 2 diabetes therapeutic agents. Expert Opin. Ther. Pat. 2008, 18, 759-768.
-
(2008)
Expert Opin. Ther. Pat.
, vol.18
, pp. 759-768
-
-
Sarabu, R.1
Berthel, S.J.2
Kester, R.F.K.3
Tilley, J.W.T.4
-
3
-
-
59149101384
-
Glucokinase activators for the potential treatment of type 2 diabetes
-
Grimsby, J.; Berthel, S. J.; Sarabu, R. Glucokinase activators for the potential treatment of type 2 diabetes. Curr. Top. Med. Chem. 2008, 8, 1524-1532.
-
(2008)
Curr. Top. Med. Chem.
, vol.8
, pp. 1524-1532
-
-
Grimsby, J.1
Berthel, S.J.2
Sarabu, R.3
-
4
-
-
16244376651
-
-
Matschinsky, F. M., Magnuson, M. A., Eds.; Karger Publishers: Basel, Switzerland
-
Van Schaftingen, E.; Veigha da Cunha, M. In Frontiers in Diabetes; Matschinsky, F. M., Magnuson, M. A., Eds.; Karger Publishers: Basel, Switzerland, 2004; Vol.16, pp 193-207.
-
(2004)
Frontiers in Diabetes
, vol.16
, pp. 193-207
-
-
Van Schaftingen, E.1
Veigha Da Cunha, M.2
-
5
-
-
0028108819
-
Short-term regulation of glucokinase
-
Van Shaftingen, E. Short-term regulation of glucokinase. Diabetologia 1994, 37, S43-47.
-
(1994)
Diabetologia
, vol.37
-
-
Van Shaftingen, E.1
-
6
-
-
0037624071
-
Allosteric activators of glucokinase: Potential role in diabetes therapy
-
Grimsby, J.; Sarabu, R.; Corbett, W. L.; Haynes, N. E.; Bizzarro, F. T.; Coffey, J. W.; Guertin, K. R.; Hilliard, D. W.; Kester, R. F.; Mahaney, P. E.; Marcus, L.; Qi, L.; Spence, C. L.; Tengi, J.; Magnuson, M. A.; Chu, C. A.; Dvorozniak, M. T.; Matschinsky, F. M.; Grippo, J. F. Allosteric activators of glucokinase: Potential role in diabetes therapy. Science 2003, 301, 370.
-
(2003)
Science
, vol.301
, pp. 370
-
-
Grimsby, J.1
Sarabu, R.2
Corbett, W.L.3
Haynes, N.E.4
Bizzarro, F.T.5
Coffey, J.W.6
Guertin, K.R.7
Hilliard, D.W.8
Kester, R.F.9
Mahaney, P.E.10
Marcus, L.11
Qi, L.12
Spence, C.L.13
Tengi, J.14
Magnuson, M.A.15
Chu, C.A.16
Dvorozniak, M.T.17
Matschinsky, F.M.18
Grippo, J.F.19
-
7
-
-
14644396894
-
-
Matschinsky, F. M., Magnuson, M. A., Eds.; Karger Publishers: Basel, Switzerland
-
Grimsby, J.; Matschinsky, F. M.; Grippo, J. F. In Frontiers in Diabetes; Matschinsky, F. M., Magnuson, M. A., Eds.; Karger Publishers: Basel, Switzerland, 2004; Vol.16, pp360-378.
-
(2004)
Frontiers in Diabetes
, vol.16
, pp. 360-378
-
-
Grimsby, J.1
Matschinsky, F.M.2
Grippo, J.F.3
-
8
-
-
70349649145
-
-
Utilizing standard chlorosulfonic acid conditions (-0°C to RT) gave the para/meta mixture, while reaction at lower temperatures (-78°C) resulted in only sulfonic acid, which upon warming resulted in the same 80:20 mixture. Heating the reaction to 75°C as well did not alter the product ratio but instead decomposed. Fluorosulfonic acid as well as standard nitration methods gave identical outcomes
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Utilizing standard chlorosulfonic acid conditions (-0°C to RT) gave the para/meta mixture, while reaction at lower temperatures (-78°C) resulted in only sulfonic acid, which upon warming resulted in the same 80:20 mixture. Heating the reaction to 75°C as well did not alter the product ratio but instead decomposed. Fluorosulfonic acid as well as standard nitration methods gave identical outcomes.
-
-
-
-
9
-
-
0017611302
-
Indancarboxylic acids, I. Electrophilic substitution reactions of 1-indancarboxylic acid and synthesis of 6-substituted 1-indancarboxylic acids as potential antiinflammatory agents
-
Aono, T.; Kishimoto, S.; Araki, Y.; Noguchi, S. Indancarboxylic acids, I. Electrophilic substitution reactions of 1-indancarboxylic acid and synthesis of 6-substituted 1-indancarboxylic acids as potential antiinflammatory agents. Chem. Pharm. Bull. 1977, 25 (12), 3198.
-
(1977)
Chem. Pharm. Bull.
, vol.25
, Issue.12
, pp. 3198
-
-
Aono, T.1
Kishimoto, S.2
Araki, Y.3
Noguchi, S.4
-
10
-
-
1542457784
-
Synthesis of p-alkylphenylacetic acids
-
o:m:p ratio 4:38:58
-
Morgan E. D. Synthesis of p-alkylphenylacetic acids. Tetrahedron 1967, 23, 1735-1738; o:m:p ratio 4:38:58.
-
(1967)
Tetrahedron
, vol.23
, pp. 1735-1738
-
-
Morgan, E.D.1
-
11
-
-
27644544833
-
5 supported on silica gel- a useful reagent for the nitration of aromatic compounds under solvent-free conditions
-
5 supported on silica gel- a useful reagent for the nitration of aromatic compounds under solvent-free conditions. Tetrahedron Lett. 2005, 46, 8307-8310.
-
(2005)
Tetrahedron Lett.
, vol.46
, pp. 8307-8310
-
-
Hajipour, A.R.1
Ruoho, A.E.2
-
12
-
-
60349091506
-
Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady State Enzyme Systems
-
Wiley classics library ed., Wiley: New York
-
Segal I. H. Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady State Enzyme Systems. In Rapid Equilibrium Partial and Mixed-Type Inhibition, Wiley classics library ed., Wiley: New York, 1993; pp 189-192.
-
(1993)
Rapid Equilibrium Partial and Mixed-Type Inhibition
, pp. 189-192
-
-
Segal, I.H.1
-
13
-
-
0029851722
-
Evidence for a role of glucose-induced translocation of glucokinase in the control of hepatic glycogen synthesis
-
Agius, L.; Peak, M.; Newgard, C. B.; Gomez-Foix, A. M.; Guinovart, J. J. Evidence for a role of glucose-induced translocation of glucokinase in the control of hepatic glycogen synthesis. J. Biol. Chem. 1996, 271, 30479-30486.
-
(1996)
J. Biol. Chem.
, vol.271
, pp. 30479-30486
-
-
Agius, L.1
Peak, M.2
Newgard, C.B.3
Gomez-Foix, A.M.4
Guinovart, J.J.5
-
14
-
-
33644895842
-
The rise of PAMPA
-
compounds are measured at 5-10 μMin 96-well filter plates coated with a hexadecane membrane. Transport is measured at 3 pH values in line with the gastrointestinal tract, and permeability is quantified by LC/MS
-
Avdeef, A. The rise of PAMPA. Expert Opin. Drug Metab. Toxicol. 2005, 1 (2), 325-342; compounds are measured at 5-10 μMin 96-well filter plates coated with a hexadecane membrane. Transport is measured at 3 pH values in line with the gastrointestinal tract, and permeability is quantified by LC/MS.
-
(2005)
Expert Opin. Drug Metab. Toxicol.
, vol.1
, Issue.2
, pp. 325-342
-
-
Avdeef, A.1
-
15
-
-
70349641928
-
-
GI values of >5.1 correspond to a low rating (estimated <35% absorbed)
-
GI values of >5.1 correspond to a low rating (estimated <35% absorbed).
-
-
-
-
16
-
-
36849049288
-
Development of a high throughput equilibrium solubility assay using miniaturized shakeflask method in early drug discovery
-
the HT-equilibrium solubility assay utilizes a novel miniaturized shake-flask approach and streamlined HPLC analysis, and is a fast, reliable, and cost-effective screening tool for solubility assessment in early drug discovery
-
Zhou, L.; Yang, L.; Tilton, S.; Wang, J. Development of a high throughput equilibrium solubility assay using miniaturized shakeflask method in early drug discovery. J. Pharm. Sci. 2007, 96 (11), 3052-3071; the HT-equilibrium solubility assay utilizes a novel miniaturized shake-flask approach and streamlined HPLC analysis, and is a fast, reliable, and cost-effective screening tool for solubility assessment in early drug discovery.
-
(2007)
J. Pharm. Sci.
, vol.96
, Issue.11
, pp. 3052-3071
-
-
Zhou, L.1
Yang, L.2
Tilton, S.3
Wang, J.4
-
17
-
-
0036846773
-
The use of in vitro metabolic stability for rapid selection of compounds in early discovery based on their expected hepatic extraction ratios
-
metabolic clearance using liver microsomes with or without specific enzyme cofactors (NADPH, UDPGA). Compounds are incubated at 1 μM in 96-well assay plates with liver microsomes + selected cofactors. Clearance is measured at 4 time points, and % test compound remaining vs. time is used to calculate clearance.
-
Lau, Y. Y.; Krishna, G.; Yumibe, N. P.; Grotz, D. E.; Sapidou, E.; Norton, L.; Chu, I.; Chen, C.; Soares, A. D.; Lin, C. C. The use of in vitro metabolic stability for rapid selection of compounds in early discovery based on their expected hepatic extraction ratios. Pharm. Res. 2002, 19, 1606-1610; metabolic clearance using liver microsomes with or without specific enzyme cofactors (NADPH, UDPGA). Compounds are incubated at 1 μM in 96-well assay plates with liver microsomes + selected cofactors. Clearance is measured at 4 time points, and % test compound remaining vs. time is used to calculate clearance.
-
(2002)
Pharm. Res.
, vol.19
, pp. 1606-1610
-
-
Lau, Y.Y.1
Krishna, G.2
Yumibe, N.P.3
Grotz, D.E.4
Sapidou, E.5
Norton, L.6
Chu, I.7
Chen, C.8
Soares, A.D.9
Lin, C.C.10
-
18
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70349646838
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Racemic materials were employed including racemic 2a for comparison
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Racemic materials were employed including racemic 2a for comparison.
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19
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70349648446
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Equilibrium solubility for all compounds in this article were <0.003 g/L unless otherwise stated
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Equilibrium solubility for all compounds in this article were <0.003 g/L unless otherwise stated.
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70349647545
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Microemulsion vehicle is defined as Cremophor RH40 (43%), corn oil-monodiglyceride (35.75), propylene glycol (10.6%), and ethanol(10.6%). This vehicle is then diluted with water in a 2-part microemulsion/3 part water as the compound is dissolved in it
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Microemulsion vehicle is defined as Cremophor RH40 (43%), corn oil-monodiglyceride (35.75), propylene glycol (10.6%), and ethanol(10.6%). This vehicle is then diluted with water in a 2-part microemulsion/3 part water as the compound is dissolved in it.
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70349640973
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Separation was accomplished on a proprietary chiral column similar to the ChiralPak IA column using simulated moving bed chromatography with 50:40:10 n-hexane/ethyl acetate/ methanol
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Separation was accomplished on a proprietary chiral column similar to the ChiralPak IA column using simulated moving bed chromatography with 50:40:10 n-hexane/ethyl acetate/ methanol.
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-
-
-
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-
1542791635
-
Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase
-
DOI 10.1016/j.str.2004.02.005, PII S0969212604000474
-
Kamata, K.; Mitsuya, M.; Nishimura, T.; Eiki, J.; Nagata, Y. Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase. Structure 2004, 12, 429-438. (Pubitemid 38353064)
-
(2004)
Structure
, vol.12
, Issue.3
, pp. 429-438
-
-
Kamata, K.1
Mitsuya, M.2
Nishimura, T.3
Eiki, J.-I.4
Nagata, Y.5
-
23
-
-
23844550012
-
A novel glucokinase activator modulates pancreatic islet and hepatocyte function
-
DOI 10.1210/en.2005-0377
-
Efanov, A. M.; Barrett, D. G.; Brenner, M. B.; Briggs, S. L.; Delaunois, A.; Durbin, J. D.; Giese, U.; Guo, H.; Radloff, M.; Gill, G. S.; Sewing, S.; Wang, Y.; Weichert, A.; Zaliani, A.; Gromada, J. A novel glucokinase activator modulates pancreatic islet and hepatocyte function. Endocrinology 2005, 146, 3696-3701. (Pubitemid 41175734)
-
(2005)
Endocrinology
, vol.146
, Issue.9
, pp. 3696-3701
-
-
Efanov, A.M.1
Barrett, D.G.2
Brenner, M.B.3
Briggs, S.L.4
Delaunois, A.5
Durbin, J.D.6
Giese, U.7
Guo, H.8
Radloff, M.9
Gil, G.S.10
Sewing, S.11
Wang, Y.12
Weichert, A.13
Zaliani, A.14
Gromada, J.15
-
24
-
-
70349643947
-
The novel glucokinase activator LBX192 stably reverses diabetes and obesity, prevents liver steatosis and increases energy expenditure in diet-inducted obese mice
-
submitted
-
Duttaroy, A.; Caplan, S.; Bebernitz, G.; Chau, M.; Crowe, H.; Dubiel, D.; Gao, J.; Joly, E.; Kavana, M.; Madiraju, M.; Taslimi, P.; Zhang, X.; Prentki, M.; Gromada, J. The novel glucokinase activator LBX192 stably reverses diabetes and obesity, prevents liver steatosis and increases energy expenditure in diet-inducted obese mice, Diabetes, submitted.
-
Diabetes
-
-
Duttaroy, A.1
Caplan, S.2
Bebernitz, G.3
Chau, M.4
Crowe, H.5
Dubiel, D.6
Gao, J.7
Joly, E.8
Kavana, M.9
Madiraju, M.10
Taslimi, P.11
Zhang, X.12
Prentki, M.13
Gromada, J.14
-
25
-
-
0018144124
-
Glucose phosphorylation, glucose-6-phosphatase, and recycling in rat hepatocytes
-
Katz, J.; Wals, P. A.; Rognstad, R. Glucose phosphorylation, glucose-6-phosphatase, and recycling in rat hepatocytes. J. Biol. Chem. 1978, 253, 4530-4536.
-
(1978)
J. Biol. Chem.
, vol.253
, pp. 4530-4536
-
-
Katz, J.1
Wals, P.A.2
Rognstad, R.3
-
26
-
-
0014645531
-
High-yield preparation of isolated rat liver parenchymal cells: A biochemical and fine structural study
-
Berry, M. N.; Friend, D. S. High-yield preparation of isolated rat liver parenchymal cells: a biochemical and fine structural study. J. Cell Biol. 1969, 43, 506-520.
-
(1969)
J. Cell Biol.
, vol.43
, pp. 506-520
-
-
Berry, M.N.1
Friend, D.S.2
-
27
-
-
0034163785
-
Investigation of the mechanism by which glucose analogues cause translocation of glucokinase in hepatocytes: Evidence for two glucose binding sites
-
DOI 10.1042/0264-6021:3460413
-
Agius, L.; Stubbs, M. Investigation of the mechanism by which glucose analogues cause translocation of glucokinase in hepatocytes: evidence for two glucose binding sites. Biochem. J. 2000, 346, 413-421. (Pubitemid 30148128)
-
(2000)
Biochemical Journal
, vol.346
, Issue.2
, pp. 413-421
-
-
Agius, L.1
Stubbs, M.2
-
28
-
-
0031059866
-
Processing of X-ray Diffraction Data Collected in Oscillation Mode
-
Carter, C.W., Jr., Sweet, R. M., Eds., Academic Press: New York, Macromolecular Crystallography, part A
-
Otwinowski, Z.; Minor, W. Processing of X-ray Diffraction Data Collected in Oscillation Mode. Methods in Enzymology; Carter, C.W., Jr., Sweet, R. M., Eds., Academic Press: New York, 1985; Vol.276, Macromolecular Crystallography, part A, pp 307-326.
-
(1985)
Methods in Enzymology
, vol.276
, pp. 307-326
-
-
Otwinowski, Z.1
Minor, W.2
-
29
-
-
32644466127
-
Likelihood enhanced fast rotation functions
-
Storoni, L. C.; McCoy, A. J.; Read, R. J. Likelihood enhanced fast rotation functions. Acta Crystallogr., Sect. D 2004, 59, 1145-11115
-
(2004)
Acta Crystallogr., Sect. D
, vol.59
, pp. 1145-11115
-
-
Storoni, L.C.1
McCoy, A.J.2
Read, R.J.3
-
30
-
-
3543012707
-
Crystallography and NMR system (CNS): A new software system for macromolecular structure determination
-
Brunger, A. T.; Adams, P. D.; Clore, G. M.; DeLano, W. L.; Gros, P.; Grosse-Kunstleve, R. W.; Jiang, J. S.; Kuszewski, J.; Nilges, N.; Pannu, N. S.; Read, R. J.; Rice, L. M.; Simonson, T.; Warren, G. L. Crystallography and NMR system (CNS): A new software system for macromolecular structure determination. Acta Crystallogr., Sect. D 1998, 54, 905-921.
-
(1998)
Acta Crystallogr., Sect. D
, vol.54
, pp. 905-921
-
-
Brunger, A.T.1
Adams, P.D.2
Clore, G.M.3
DeLano, W.L.4
Gros, P.5
Grosse-Kunstleve, R.W.6
Jiang, J.S.7
Kuszewski, J.8
Nilges, N.9
Pannu, N.S.10
Read, R.J.11
Rice, L.M.12
Simonson, T.13
Warren, G.L.14
-
31
-
-
13244281317
-
Coot: Model-Building Tools for Molecular Graphics
-
Emsley, P.; Cowton, K. Coot: Model-Building Tools for Molecular Graphics. Acta Crystallogr., Sect. D 2004, 60, 2126-2132.
-
(2004)
Acta Crystallogr., Sect. D
, vol.60
, pp. 2126-2132
-
-
Emsley, P.1
Cowton, K.2
|