3IMX
| Crystal Structure of human glucokinase in complex with a synthetic activator | Descriptor: | (2R)-3-cyclopentyl-N-(5-methoxy[1,3]thiazolo[5,4-b]pyridin-2-yl)-2-{4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}propanamide, Glucokinase, SODIUM ION, ... | Authors: | Stams, T, Vash, B. | Deposit date: | 2009-08-11 | Release date: | 2009-10-06 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J.Med.Chem., 52, 2009
|
|
3A0I
| Human glucokinase in complex with a synthetic activator | Descriptor: | 3-[(4-fluorophenyl)sulfanyl]-N-(4-methyl-1,3-thiazol-2-yl)-6-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]pyridine-2-carboxamide, Glucokinase, SODIUM ION, ... | Authors: | Kamata, K, Mitsuya, M. | Deposit date: | 2009-03-19 | Release date: | 2009-04-28 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators Bioorg.Med.Chem.Lett., 19, 2009
|
|
4RCH
| Discovery of 2-Pyridyl Ureas as Glucokinase Activators | Descriptor: | 1-{3-[(2-ethylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}-3-methylurea, Glucokinase, alpha-D-glucopyranose | Authors: | Voegtli, W, Vigers, G.P.A. | Deposit date: | 2014-09-16 | Release date: | 2014-10-08 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Discovery of 2-pyridylureas as glucokinase activators. J.Med.Chem., 57, 2014
|
|
3QIC
| The structure of human glucokinase E339K mutation | Descriptor: | GLYCEROL, Glucokinase, alpha-D-glucopyranose | Authors: | Liu, Q, Liu, S, Liu, J. | Deposit date: | 2011-01-27 | Release date: | 2011-06-01 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Crystal structure of E339K mutated human glucokinase reveals changes in the ATP binding site. Febs Lett., 585, 2011
|
|
4MLE
| Human Glucokinase in Complex with Novel Amino Thiazole Activator | Descriptor: | 3-(benzyloxy)-N-(4-methyl-1,3-thiazol-2-yl)pyridin-2-amine, Glucokinase, alpha-D-glucopyranose | Authors: | Voegtli, W.C. | Deposit date: | 2013-09-06 | Release date: | 2013-09-25 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Identification of a New Class of Glucokinase Activators through Structure-Based Design. J.Med.Chem., 56, 2013
|
|
4MLH
| |
4DHY
| Crystal structure of human glucokinase in complex with glucose and activator | Descriptor: | Glucokinase, N,N-dimethyl-5-({2-methyl-6-[(5-methylpyrazin-2-yl)carbamoyl]-1-benzofuran-4-yl}oxy)pyrimidine-2-carboxamide, SODIUM ION, ... | Authors: | Liu, S. | Deposit date: | 2012-01-30 | Release date: | 2012-02-08 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.38 Å) | Cite: | Insights into Mechanism of Glucokinase Activation: OBSERVATION OF MULTIPLE DISTINCT PROTEIN CONFORMATIONS. J.Biol.Chem., 287, 2012
|
|
4DCH
| Insights into Glucokinase Activation Mechanism: Observation of Multiple Distinct Protein Conformations | Descriptor: | (2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide, Glucokinase, IODIDE ION, ... | Authors: | Greasley, S.E, Hickey, M, Feng, J, Garcia, E. | Deposit date: | 2012-01-17 | Release date: | 2012-02-08 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.79 Å) | Cite: | Insights into Mechanism of Glucokinase Activation: OBSERVATION OF MULTIPLE DISTINCT PROTEIN CONFORMATIONS. J.Biol.Chem., 287, 2012
|
|
6E0I
| Crystal structure of Glucokinase in complex with compound 72 | Descriptor: | 1-{4-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-[(pyridin-2-yl)sulfanyl]pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]piperidin-1 -yl}ethan-1-one, DIMETHYL SULFOXIDE, Glucokinase, ... | Authors: | Hinklin, R.J, Baer, B.R, Boyd, S.A, Chicarelli, M.D, Condroski, K.R, DeWolf, W.E, Fischer, J, Frank, M, Hingorani, G.P, Lee, P.A, Neitzel, N.A, Pratt, S.A, Singh, A, Sullivan, F.X, Turner, T, Voegtli, W.C, Wallace, E.M, Williams, L, Aicher, T.D. | Deposit date: | 2018-07-06 | Release date: | 2019-07-10 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorg.Med.Chem., 28, 2020
|
|
6E0E
| Crystal structure of Glucokinase in complex with compound 6 | Descriptor: | 2-({2-[(4-methyl-1,3-thiazol-2-yl)amino]pyridin-3-yl}oxy)benzonitrile, Glucokinase, alpha-D-glucopyranose | Authors: | Hinklin, R.J, Baer, B.R, Boyd, S.A, Chicarelli, M.D, Condroski, K.R, DeWolf, W.E, Fischer, J, Frank, M, Hingorani, G.P, Lee, P.A, Neitzel, N.A, Pratt, S.A, Singh, A, Sullivan, F.X, Turner, T, Voegtli, W.C, Wallace, E.M, Williams, L, Aicher, T.D. | Deposit date: | 2018-07-06 | Release date: | 2019-07-10 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorg.Med.Chem., 28, 2020
|
|
5V4X
| Human glucokinase in complex with novel pyrazole activator. | Descriptor: | (2S)-3-cyclohexyl-2-[4-(cyclopentylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(1,3-thiazol-2-yl)propanamide, Glucokinase, IODIDE ION, ... | Authors: | Skene, R.J, Hosfiled, D.J. | Deposit date: | 2017-03-10 | Release date: | 2017-05-31 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.08 Å) | Cite: | Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorg. Med. Chem. Lett., 27, 2017
|
|
7T79
| |
7T78
| |
1V4T
| Crystal structure of human glucokinase | Descriptor: | SODIUM ION, SULFATE ION, glucokinase isoform 2 | Authors: | Kamata, K, Mitsuya, M, Nishimura, T, Eiki, J, Nagata, Y. | Deposit date: | 2003-11-19 | Release date: | 2004-03-30 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (3.4 Å) | Cite: | Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase Structure, 12, 2004
|
|
5V4W
| Human glucokinase in complex with novel indazole activator. | Descriptor: | (2S)-2-[4-(cyclopropylsulfonyl)-1H-indazol-1-yl]-N-(5-fluoro-1,3-thiazol-2-yl)-3-(oxan-4-yl)propanamide, Glucokinase, IODIDE ION, ... | Authors: | Skene, R.J, Hosfield, D.J. | Deposit date: | 2017-03-10 | Release date: | 2017-05-31 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.39 Å) | Cite: | Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorg. Med. Chem. Lett., 27, 2017
|
|
1V4S
| Crystal structure of human glucokinase | Descriptor: | 2-AMINO-4-FLUORO-5-[(1-METHYL-1H-IMIDAZOL-2-YL)SULFANYL]-N-(1,3-THIAZOL-2-YL)BENZAMIDE, SODIUM ION, alpha-D-glucopyranose, ... | Authors: | Kamata, K, Mitsuya, M, Nishimura, T, Eiki, J, Nagata, Y. | Deposit date: | 2003-11-19 | Release date: | 2004-03-30 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase Structure, 12, 2004
|
|
3FR0
| Human glucokinase in complex with 2-amino benzamide activator | Descriptor: | 2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide, Glucokinase, SODIUM ION, ... | Authors: | Kamata, K. | Deposit date: | 2009-01-08 | Release date: | 2009-02-17 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators Bioorg.Med.Chem.Lett., 19, 2009
|
|
4NO7
| Human Glucokinase in complex with a nanomolar activator. | Descriptor: | (2R)-2-[3-chloro-4-(methylsulfonyl)phenyl]-3-[(1R)-3-oxocyclopentyl]-N-(pyrazin-2-yl)propanamide, Glucokinase, alpha-D-glucopyranose | Authors: | Petit, P, Ferry, G, Antoine, M, Boutin, J.A, Kotschy, A, Perron-Sierra, F, Mamelli, L, Vuillard, L. | Deposit date: | 2013-11-19 | Release date: | 2014-10-29 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | The active conformation of human glucokinase is not altered by allosteric activators. Acta Crystallogr. D Biol. Crystallogr., 67, 2011
|
|
3F9M
| Human pancreatic glucokinase in complex with glucose and activator showing a mobile flap | Descriptor: | 2-AMINO-4-FLUORO-5-[(1-METHYL-1H-IMIDAZOL-2-YL)SULFANYL]-N-(1,3-THIAZOL-2-YL)BENZAMIDE, Glucokinase, alpha-D-glucopyranose | Authors: | Petit, P, Gluais, L, Lagarde, A, Vuillard, L, Boutin, J.A, Ferry, G. | Deposit date: | 2008-11-14 | Release date: | 2008-12-02 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (1.5 Å) | Cite: | The active conformation of human glucokinase is not altered by allosteric activators Acta Crystallogr.,Sect.D, 67, 2011
|
|
3FGU
| Catalytic complex of Human Glucokinase | Descriptor: | Glucokinase, MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, ... | Authors: | Petit, P, Lagarde, A, Boutin, J.A, Ferry, G, Vuillard, L. | Deposit date: | 2008-12-08 | Release date: | 2009-12-15 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | The active conformation of human glucokinase is not altered by allosteric activators Acta Crystallogr.,Sect.D, 67, 2011
|
|
3S41
| Glucokinase in complex with activator and glucose | Descriptor: | Glucokinase, N,N-dimethyl-5-({2-methyl-6-[(5-methylpyrazin-2-yl)carbamoyl]-1-benzofuran-4-yl}oxy)pyrimidine-2-carboxamide, SODIUM ION, ... | Authors: | Liu, S. | Deposit date: | 2011-05-18 | Release date: | 2011-09-14 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (2.18 Å) | Cite: | Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus MEDCHEMCOMM, 2, 2011
|
|
3VF6
| Glucokinase in complex with glucose and activator | Descriptor: | 6-({(2S)-3-cyclopentyl-2-[4-(trifluoromethyl)-1H-imidazol-1-yl]propanoyl}amino)pyridine-3-carboxylic acid, Glucokinase, SODIUM ION, ... | Authors: | Liu, S. | Deposit date: | 2012-01-09 | Release date: | 2012-02-08 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.86 Å) | Cite: | Insights into Mechanism of Glucokinase Activation: OBSERVATION OF MULTIPLE DISTINCT PROTEIN CONFORMATIONS. J.Biol.Chem., 287, 2012
|
|
3VEY
| glucokinase in complex with glucose and ATPgS | Descriptor: | 6-methoxy-N-(1-methyl-1H-pyrazol-3-yl)quinazolin-4-amine, Glucokinase, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, ... | Authors: | Liu, S. | Deposit date: | 2012-01-09 | Release date: | 2012-02-08 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (2.25 Å) | Cite: | Insights into Mechanism of Glucokinase Activation: OBSERVATION OF MULTIPLE DISTINCT PROTEIN CONFORMATIONS. J.Biol.Chem., 287, 2012
|
|
3VEV
| Glucokinase in complex with an activator and glucose | Descriptor: | (2S)-3-cyclopentyl-N-(5-methylpyridin-2-yl)-2-[2-oxo-4-(trifluoromethyl)pyridin-1(2H)-yl]propanamide, Glucokinase, SODIUM ION, ... | Authors: | Liu, S. | Deposit date: | 2012-01-09 | Release date: | 2012-02-08 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Insights into Mechanism of Glucokinase Activation: OBSERVATION OF MULTIPLE DISTINCT PROTEIN CONFORMATIONS. J.Biol.Chem., 287, 2012
|
|
3GOI
| Human glucokinase in complex with a synthetic activator | Descriptor: | 2-(methylamino)-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide, Glucokinase, alpha-D-glucopyranose | Authors: | Kamata, K, Mitsuya, M. | Deposit date: | 2009-03-19 | Release date: | 2009-04-28 | Last modified: | 2024-03-20 | Method: | X-RAY DIFFRACTION (2.52 Å) | Cite: | Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators Bioorg.Med.Chem.Lett., 19, 2009
|
|