- ►diabetesjournals.org D Johnson, RM Shepherd, D Gill, T Gorman, … - Diabetes, 2007 - Am Diabetes Assoc Because glucokinase is a metabolic sensor involved in the regulated release of
insulin, we have investigated the acute actions of novel glucokinase activator
compound 50 (GKA50) on islet function. Insulin secretion was determined by ... Cited by 15 - Related articles - BL Direct - All 6 versions
MCT Fyfe, JR White, A Taylor, R Chatfield, E … - Diabetologia, 2007 - Springer Abstract Aims/hypothesis We evaluated the insulinotropic and anti-
hyperglycaemic actions of glucokinase activators (GKAs), especially through
acute and subchronic studies in rodent diabetes models with (2R)-2-(4- ... Cited by 12 - Related articles - BL Direct - All 5 versions
D McKerrecher, JV Allen, PWR Caulkett, CS … - Bioorganic & medicinal chemistry letters, 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 ... Cited by 26 - Related articles - All 6 versions
GJ Coope, AM Atkinson, C Allott, D … - British journal of pharmacology, 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 ... Cited by 18 - Related articles - BL Direct - All 4 versions
- ►shouxi.net M Futamura, H Hosaka, A Kadotani, H … - Journal of Biological Chemistry, 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 ... Cited by 25 - Related articles - All 7 versions
D Mckerrecher, JV Allen, SS Bowker, S Boyd, … - Bioorganic & medicinal chemistry letters, 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 ... Cited by 20 - Related articles - All 4 versions
AL Castelhano, H Dong, MCT Fyfe, LS Gardner … - Bioorganic & Medicinal Chemistry Letters, 2005 - Elsevier Glucokinase (GK) is the characteristic hexokinase isoenzyme found in hepatocytes
and in pancreatic β-cells. 1 This enzyme catalyses the first step in glucose
(Glc) metabolism, viz., the conversion of Glc to glucose-6-phosphate. As ... Cited by 17 - Related articles - All 4 versions
B Leighton, A Atkinson, M Coghlan - Biochemical Society Transactions, 2005 - bst.portlandpress.com The monomeric enzyme GK (glucokinase) has a low affinity for glucose and,
quantitatively, is largely expressed in the liver and pancreatic b-cells,
playing a key 'glucose sensing' role to regulate hepatic glucose balance ... Cited by 17 - Related articles - Cached - All 10 versions
M Coghlan, B Leighton - Expert Opin. Investig. Drugs, 2008 - informahealthcare.com Type 2 diabetes is a chronic metabolic disease that adversely affects both the
quality and longevity of life. The disease is characterised by elevated blood
glucose (hyperglycaemia) that is associated with microvascular ... Cited by 12 - Related articles - BL Direct - All 6 versions
J Grimsby, FM Matschinsky, JF Grippo - Glucokinase and Glycemic Disease: From Basics to … - books.google.com Fig. 3. Close-up of GKA binding site showing amino acid residues making direct
interactions with a GKA. Mutations in V62, M210 and M235 cause the MODY-2 pheno-
type whereas V455M, A456V and Y214A mutations increase the catalytic ... Cited by 21 - Related articles - BL Direct - All 3 versions
