KJ Brocklehurst, VA Payne, RA Davies, D Carroll, HL … - Diabetes, 2004 - Am Diabetes Assoc Glucokinase (GK) has a major role in the control of blood glucose homeostasis and is a strong
potential target for the pharmacological treatment of type 2 diabetes. We report here the mechanism
of action of two novel and potent direct activators of GK: 6-[(3-isobutoxy-5- ... Cited by 76 - Related articles - BL Direct - All 6 versions
- ►sciencesignaling.org [PDF] J Grimsby, R Sarabu, WL Corbett, NE Haynes, FT … - Science, 2003 - sciencemag.org Page 1. DOI: 10.1126/science.1084073 , 370 (2003); 301 Science et al. Joseph
Grimsby, in Diabetes Therapy Allosteric Activators of Glucokinase: Potential Role
www.sciencemag.org (this information is current as of January ... Cited by 187 - Related articles - All 12 versions
- ►cell.com K Kamata, M Mitsuya, T Nishimura, J Eiki, Y Nagata - Structure, 2004 - Elsevier Glucokinase is a monomeric enzyme that displays a low affinity for glucose and a sigmoidal saturation
curve for its substrate, two properties that are important for its playing the role of a glucose sensor
in pancreas and liver. The molecular basis for these two properties is not well understood. ... Cited by 127 - Related articles - All 10 versions
- ►endojournals.org AM Efanov, DG Barrett, MB Brenner, SL Briggs, A … - Endocrinology, 2005 - Endocrine Soc The glucose-sensing enzyme glucokinase (GK) plays a key role in glucose metabolism. We report
here the effects of a novel glucokinase activator, LY2121260. The activator enhanced GK activity
via binding to the allosteric site located in the hinge region of the enzyme. LY2121260 ... Cited by 56 - Related articles - BL Direct - All 5 versions
- ►jbc.org S Baltrusch, S Lenzen, DA Okar, AJ Lange, M … - Journal of Biological …, 2001 - ASBMB The low affinity glucose-phosphorylating enzyme glucokinase shows the phenomenon of intracellular
translocation in beta cells of the pancreas and the liver. To identify potential binding partners
of glucokinase by a systematic strategy, human beta cell glucokinase was screened by a ... Cited by 46 - Related articles - BL Direct - All 4 versions
M Futamura, H Hosaka, A Kadotani, H Shimazaki, K … - Journal of Biological …, 2006 - ASBMB Glucokinase (GK) plays a key role in the control of blood glucose homeostasis. We identified
a small molecule GK activator, compound A, that increased the glucose affinity and maximal
velocity (V max ) of GK. Compound A augmented insulin secretion from isolated rat islets ... Cited by 25 - Related articles - All 7 versions
D McKerrecher, JV Allen, PWR Caulkett, CS … - Bioorganic & medicinal …, 2006 - Elsevier The optimisation of a series of glucokinase activators is described, including attempts to uncouple
the relationship between potency and plasma protein binding, and to better understand the key
pharmacokinetic properties of the series. The use of unbound clearance as an ... Cited by 26 - Related articles - All 6 versions
- ►diabetesjournals.org VA Payne, C Arden, C Wu, AJ Lange, L Agius - Diabetes, 2005 - Am Diabetes Assoc Hepatic glucokinase is regulated by a 68-kDa regulatory protein (GKRP) that is both an inhibitor
and nuclear receptor for glucokinase. We tested the role of 6-phosphofructo-2-kinase/fructose
-2,6-bisphosphatase (PFK2) in regulating glucokinase compartmentation in hepatocytes. ... Cited by 29 - Related articles - All 5 versions
GJ Coope, AM Atkinson, C Allott, D … - British journal of …, 2006 - pubmedcentral.nih.gov Four GKAs (at 1 to 30 mg kg −1 ), with different in vitro enzyme potencies, dose-dependently
improved oral glucose tolerance in HFFZ rats (10–40% decrease glucose area under the curve
(AUC) from vehicle control). The extent of glucose lowering, or the pharmacodynamic ... Cited by 18 - Related articles - BL Direct - All 4 versions
D Mckerrecher, JV Allen, SS Bowker, S Boyd, PWR … - Bioorganic & medicinal …, 2005 - Elsevier The elevated blood glucose levels that characterise type 2 diabetes result from a combination
of defects in hepatic glucose balance and the failure of pancreatic β-cells to secrete sufficient
insulin to overcome insulin resistance. Glucokinase (GK) is the rate-limiting enzyme for ... Cited by 20 - Related articles - All 4 versions
