GK (glucokinase) catalyses the phosphorylation of glucose to glucose 6-phosphate in glucosensitive cells. In pancreatic β-cells, this reaction is the rate-limiting step of insulin release. Recent work has led to the discovery of synthetic small-molecule activators of GK that stimulate β-cell physiology and subsequently enhance the glucose-dependent release of insulin. It is currently recognized that these compounds may represent a significant advance in the development of new agents in the treatment of diabetes. In addition, GKAs (GK activators) are emerging as reagents that are useful tools with which to probe the function of pancreatic β-cells and other glucosensitive cells. This includes providing insights into the physiology of the β-cell by helping to elucidate the kinetic cycle of GK, confirming the central role of glucose metabolism to the β-cell and highlighting subtle species-dependent differences in insulin secretion between rodent and human islets of Langerhans.
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November 2007
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Conference Article|
October 25 2007
Glucokinase activators: molecular tools for studying the physiology of insulin-secreting cells
D. Johnson;
D. Johnson
*Faculty of Life Sciences, University of Manchester, Core Technology Facility, 46 Grafton Street, Manchester M13 9NT, U.K.
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R.M. Shepherd;
R.M. Shepherd
*Faculty of Life Sciences, University of Manchester, Core Technology Facility, 46 Grafton Street, Manchester M13 9NT, U.K.
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D. Gill;
D. Gill
†AstraZeneca, Diabetes and Obesity Drug Discovery, Mereside, Alderley Park, Cheshire SK10 4TG, U.K.
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T. Gorman;
T. Gorman
†AstraZeneca, Diabetes and Obesity Drug Discovery, Mereside, Alderley Park, Cheshire SK10 4TG, U.K.
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D.M. Smith;
D.M. Smith
†AstraZeneca, Diabetes and Obesity Drug Discovery, Mereside, Alderley Park, Cheshire SK10 4TG, U.K.
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M.J. Dunne
M.J. Dunne
1
*Faculty of Life Sciences, University of Manchester, Core Technology Facility, 46 Grafton Street, Manchester M13 9NT, U.K.
1To whom correspondence should be addressed (email mark.j.dunne@manchester.ac.uk).
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Publisher: Portland Press Ltd
Received:
July 09 2007
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© The Authors Journal compilation © 2007 Biochemical Society
2007
Biochem Soc Trans (2007) 35 (5): 1208–1210.
Article history
Received:
July 09 2007
Citation
D. Johnson, R.M. Shepherd, D. Gill, T. Gorman, D.M. Smith, M.J. Dunne; Glucokinase activators: molecular tools for studying the physiology of insulin-secreting cells. Biochem Soc Trans 1 November 2007; 35 (5): 1208–1210. doi: https://doi.org/10.1042/BST0351208
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