Additive activation of glucokinase by the bifunctional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase and the chemical activator LY2121260

Biochemical Pharmacology

Volumn 83, Issue 9, 2012, Pages 1300-1306

  Baltrusch, Simone ^a,b   Schmitt, Heike ^a   Brix, Anke ^a   Langer, Sara ^a   Lenzen, Sigurd ^a  

^a HANNOVER MEDICAL SCHOOL   (Germany)

^b UNIVERSITY OF ROSTOCK   (Germany)

Author keywords

6 Phosphofructo 2 kinase fructose 2,6 bisphosphatase; Glucokinase; Glucokinase activator LY2121260; Insulin secretion; Pancreatic beta cell

Indexed keywords

2 CYCLOHEXYL 1 (4 METHANESULFONYLPHENYL)CYCLOPROPANECARBOXYLIC ACID 2 THIAZOLYLAMIDE; 6 PHOSPHOFRUCTO 2 KINASE; ENZYME ACTIVATOR; FRUCTOSE 2,6 BISPHOSPHATASE; GLUCOKINASE; GLUCOSE; INSULIN; MANNOHEPTULOSE; RECOMBINANT ENZYME; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME CONFORMATION; GEL PERMEATION CHROMATOGRAPHY; GLUCOSE METABOLISM; INSULIN RELEASE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; PRIORITY JOURNAL; PROTEIN DOMAIN;

CELL LINE; ENZYME ACTIVATION; ENZYME INHIBITORS; GLUCOKINASE; GLUCOSE; HEPTOSES; HUMANS; INSULIN; MANNOHEPTULOSE; PHOSPHOFRUCTOKINASE-2; RECOMBINANT PROTEINS; SULFONES; THIAZOLES;

EID: 84858073775     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2012.01.020     Document Type: Article

References (40)

1. F.M. Matschinsky, M.A. Magnuson, D. Zelent, T.L. Jetton, N. Doliba, and Y. Han The network of glucokinase-expressing cells in glucose homeostasis and the potential of glucokinase activators for diabetes therapy Diabetes 55 2006 1 12
2. S. Baltrusch, and M. Tiedge Glucokinase regulatory network in pancreatic {beta}-cells and liver Diabetes 55 Suppl. 2 2006 S55 S64
3. S. Lenzen Glucokinase: signal recognition enzyme for glucose-induced insulin secretion P.R. Flatt, Nutrient regulation of insulin secretion 1992 Portland Press London and Chapel Hill 101 125
4. F.M. Matschinsky Banting Lecture 1995. A lesson in metabolic regulation inspired by the glucokinase glucose sensor paradigm Diabetes 45 1996 223 241
5. L. Agius Glucokinase and molecular aspects of liver glycogen metabolism Biochem J 414 2008 1 18
6. R. St Charles, R.W. Harrison, G.I. Bell, S.J. Pilkis, and I.T. Weber Molecular model of human beta-cell glucokinase built by analogy to the crystal structure of yeast hexokinase B Diabetes 43 1994 784 791
7. L.I. Koranyi, Y. Tanizawa, C.M. Welling, D.U. Rabin, and M.A. Permutt Human islet glucokinase gene. Isolation and sequence analysis of full-length cDNA Diabetes 41 1992 807 811
8. M.L. Cardenas Kinetic behaviour of vertebrate hexokinases with emphasis on hexokinase D (IV) Biochem Soc Trans 25 1997 131 135
9. A. Cornish-Bowden, and A.C. Storer Mechanistic origin of the sigmoidal rate behaviour of rat liver hexokinase D ('glucokinase') Biochem J 240 1986 293 296
10. K. Kamata, M. Mitsuya, T. Nishimura, J. Eiki, and Y. Nagata Structural basis for allosteric regulation of the monomeric allosteric enzyme human glucokinase Structure 12 2004 429 438
11. J. Zhang, C. Li, K. Chen, W. Zhu, X. Shen, and H. Jiang Conformational transition pathway in the allosteric process of human glucokinase Proc Natl Acad Sci USA 103 2006 13368 13373
12. M. Antoine, J.A. Boutin, and G. Ferry Binding kinetics of glucose and allosteric activators to human glucokinase reveal multiple conformational states Biochemistry 48 2009 5466 5482
13. S. Baltrusch, S. Langer, L. Massa, M. Tiedge, and S. Lenzen Improved metabolic stimulus for glucose-induced insulin secretion through GK and PFK-2/FBPase-2 coexpression in insulin-producing RINm5F cells Endocrinology 147 2006 5768 5776
14. E. van Schaftingen, M. Veiga-da-Cunha, and L. Niculescu The regulatory protein of glucokinase Biochem Soc Trans 25 1997 136 140
15. S. Baltrusch, F. Francini, S. Lenzen, and M. Tiedge Interaction of glucokinase with the liver regulatory protein is conferred by leucine-asparagine motifs of the enzyme Diabetes 54 2005 2829 2837
16. S. Baltrusch, S. Lenzen, D.A. Okar, A.J. Lange, and M. Tiedge Characterization of glucokinase-binding protein epitopes by a phage-displayed peptide library. Identification of 6-phosphofructo-2-kinase/fructose-2,6- bisphosphatase as a novel interaction partner J Biol Chem 276 2001 43915 43923
17. L. Massa, S. Baltrusch, D.A. Okar, A.J. Lange, S. Lenzen, and M. Tiedge Interaction of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2) with glucokinase activates glucose phosphorylation and glucose metabolism in insulin-producing cells Diabetes 53 2004 1020 1029
18. V.A. Payne, C. Arden, C. Wu, A.J. Lange, and L. Agius Dual role of phosphofructokinase-2/fructose bisphosphatase-2 in regulating the compartmentation and expression of glucokinase in hepatocytes Diabetes 54 2005 1949 1957
19. W.E. Smith, S. Langer, C. Wu, S. Baltrusch, and D.A. Okar Molecular coordination of hepatic glucose metabolism by the 6-phosphofructo-2-kinase/ fructose-2,6-bisphosphatase:glucokinase complex Mol Endocrinol 21 2007 1478 1487
20. S. Langer, M.T. Kaminski, S. Lenzen, and S. Baltrusch Endogenous activation of glucokinase by 6-phosphofructo-2-kinase/fructose-2,6- bisphosphatase is glucose dependent Mol Endocrinol 24 2010 1988 1997
21. B. Glaser, P. Kesavan, M. Heyman, E. Davis, A. Cuesta, and A. Buchs Familial hyperinsulinism caused by an activating glucokinase mutation N Engl J Med 338 1998 226 230
22. H.B. Christesen, B.B. Jacobsen, S. Odili, C. Buettger, A. Cuesta-Munoz, and T. Hansen The second activating glucokinase mutation (A456V): implications for glucose homeostasis and diabetes therapy Diabetes 51 2002 1240 1246
23. A.L. Cuesta-Munoz, H. Huopio, T. Otonkoski, J.M. Gomez-Zumaquero, K. Nanto-Salonen, and J. Rahier Severe persistent hyperinsulinemic hypoglycemia due to a de novo glucokinase mutation Diabetes 53 2004 2164 2168
24. A.L. Gloyn, K. Noordam, M.A. Willemsen, S. Ellard, W.W. Lam, and I.W. Campbell Insights into the biochemical and genetic basis of glucokinase activation from naturally occurring hypoglycemia mutations Diabetes 52 2003 2433 2440
25. J. Grimsby, R. Sarabu, W.L. Corbett, N.E. Haynes, F.T. Bizzarro, and J.W. Coffey Allosteric activators of glucokinase: potential role in diabetes therapy Science 301 2003 370 373
26. A.M. Efanov, D.G. Barrett, M.B. Brenner, S.L. Briggs, A. Delaunois, and J.D. Durbin A novel glucokinase activator modulates pancreatic islet and hepatocyte function Endocrinology 146 2005 3696 3701
27. K.J. Brocklehurst, V.A. Payne, R.A. Davies, D. Carroll, H.L. Vertigan, and H.J. Wightman Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators Diabetes 53 2004 535 541
28. M.C. Fyfe, J.R. White, A. Taylor, R. Chatfield, E. Wargent, and R.L. Printz Glucokinase activator PSN-GK1 displays enhanced antihyperglycaemic and insulinotropic actions Diabetologia 50 2007 1277 1287
29. D. Johnson, R.M. Shepherd, D. Gill, T. Gorman, D.M. Smith, and M.J. Dunne Glucose-dependent modulation of insulin secretion and intracellular calcium ions by GKA50, a glucokinase activator Diabetes 56 2007 1694 1702
30. F.M. Matschinsky Assessing the potential of glucokinase activators in diabetes therapy Nat Rev Drug Discov 8 2009 399 416
31. M. Tiedge, U. Krug, and S. Lenzen Modulation of human glucokinase intrinsic activity by SH reagents mirrors post-translational regulation of enzyme activity Biochim Biophys Acta 1337 1997 175 190
32. E.C. Ralph, J. Thomson, J. Almaden, and S. Sun Glucose modulation of glucokinase activation by small molecules Biochemistry 47 2008 5028 5036
33. M. Futamura, H. Hosaka, A. Kadotani, H. Shimazaki, K. Sasaki, and S. Ohyama An allosteric activator of glucokinase impairs the interaction of glucokinase and glucokinase regulatory protein and regulates glucose metabolism J Biol Chem 281 2006 37668 37674
34. N. Kappler-Tanudyaya, H. Schmitt, N. Tippkotter, L. Meyer, S. Lenzen, and R. Ulber Combination of biotransformation and chromatography for the isolation and purification of mannoheptulose Biotechnol J 2 2007 692 699
35. D. Zelent, H. Najafi, S. Odili, C. Buettger, H. Weik-Collins, and C. Li Glucokinase and glucose homeostasis: proven concepts and new ideas Biochem Soc Trans 33 2005 306 310
36. S. Baltrusch, and S. Lenzen Novel insights into the regulation of the bound and diffusible glucokinase in MIN6 beta-cells Diabetes 56 2007 1305 1315
37. J.A. Kanters, A. Schouten, and M. van Bommel Structure of lactitol (4-O-beta-d-galactopyranosyl-d-glucitol) monohydrate; and artificial sweetener Acta Crystallogr C 46 Pt 12 1990 2408 2411
38. M. Uldry, and B. Thorens The SLC2 family of facilitated hexose and polyol transporters Pflugers Arch 447 2004 480 489
39. B. Thorens Molecular and cellular physiology of GLUT-2, a high-Km facilitated diffusion glucose transporter Int Rev Cytol 137 1992 209 238
40. J.G. Chediack, E. Caviedes-Vidal, V. Fasulo, L.J. Yamin, and W.H. Karasov Intestinal passive absorption of water-soluble compounds by sparrows: effect of molecular size and luminal nutrients J Comp Physiol B 173 2003 187 197