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Science, ISSN 0036-8075, 7/2003, Volume 301, Issue 5631, pp. 370 - 373
Glucokinase (GK) plays a key role in whole-body glucose homeostasis by catalyzing the phosphorylation of glucose in cells that express this enzyme, such as... 
Circles | Blood glucose | Enzymes | Hepatocytes | Homeostasis | Reports | Glucose tolerance test | Type 2 diabetes mellitus | Diabetes | Insulin | Vehicles | GLUCOSE-HOMEOSTASIS | MUTANTS | MODY-2 | MULTIDISCIPLINARY SCIENCES | LIVER | BETA-CELL | MICE | MUTATIONS | MELLITUS | Enzyme Activators - pharmacology | Islets of Langerhans - drug effects | Rats, Wistar | Stereoisomerism | Allosteric Regulation | Humans | Liver Glycogen - biosynthesis | Male | Diabetes Mellitus, Type 2 - metabolism | Insulin - blood | Keto Acids - metabolism | Dose-Response Relationship, Drug | Liver - drug effects | Islets of Langerhans - metabolism | Enzyme Activators - chemistry | Drug Evaluation, Preclinical | Insulin Secretion | Carrier Proteins | Recombinant Proteins - metabolism | Glucose Tolerance Test | Liver - metabolism | Mice, Inbred C57BL | Rats | Hypoglycemic Agents - chemistry | Glucokinase - metabolism | Hypoglycemic Agents - pharmacology | Adaptor Proteins, Signal Transducing | Insulin - metabolism | Animals | Proteins - metabolism | Glucose - metabolism | Mice, Obese | Thiazoles - chemistry | Mice | Proteins - pharmacology | Thiazoles - pharmacology | Enzyme Activation | Blood Glucose - metabolism | Diabetes Mellitus, Type 2 - drug therapy | Type 2 diabetes | Glucose metabolism | Care and treatment | Research | Glucose | Drug therapy | Metabolism | Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2014, Volume 57, Issue 19, pp. 8180 - 8186
Glucokinase (GK) is the rate-limiting step for insulin release from the pancreas in response to high levels of glucose. Flux through GK also contributes to... 
TYPE-2 DIABETES-MELLITUS | CHEMISTRY, MEDICINAL | THERAPY | Enzyme Activators - pharmacology | Glucose Tolerance Test | Animals | Mice, Inbred C57BL | Urea - analogs & derivatives | Pyridines - chemical synthesis | Pyridines - pharmacology | Glucokinase - metabolism | Drug Discovery | Enzyme Activators - chemical synthesis | Index Medicus
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 08/2012, Volume 55, Issue 16, pp. 7021 - 7036
Journal Article
Pharmaceutical Chemistry Journal, ISSN 0091-150X, 6/2018, Volume 52, Issue 3, pp. 209 - 212
A series of previously undescribed N-aryl-N′-pyridin-2-ylureas were prepared via the reaction of 2-aminopyridines with benzoyl azides and tested in vitro as... 
N -aryl- N ′ -pyridin-2-ylurea | Pharmacology/Toxicology | Pharmacy | glucokinase activators | Organic Chemistry | N-aryl-N | pyridin-2-ylurea | N-aryl-N '-pyridin-2-ylurea | PHARMACOLOGY & PHARMACY | CHEMISTRY, MEDICINAL | Type 2 diabetes | Pancreatic beta cells | Hypoglycemic agents | Isoenzymes
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 10/2017, Volume 139, pp. 128 - 152
Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of... 
N-Thiazol-2-yl-benzamides | Type 2 diabetes mellitus | Hypoglycemia | Glucokinase activators | Dyslipidemia | CHEMISTRY, MEDICINAL | MANAGEMENT | EFFICACY | THERAPY | GLUCOSE-METABOLISM | ALLOSTERIC ACTIVATORS | LIVER | CLINICAL CANDIDATE | INHIBITOR | TYPE-2 DIABETES-MELLITUS | PSN-GK1 | Enzyme Activators - pharmacology | Diabetes Mellitus, Experimental - drug therapy | Apoptosis - drug effects | Streptozocin | Male | Structure-Activity Relationship | Dose-Response Relationship, Drug | Enzyme Activators - chemistry | Benzamides - pharmacology | Diabetes Mellitus, Experimental - chemically induced | Molecular Structure | Benzamides - chemistry | Glucose Tolerance Test | Mice, Inbred C57BL | Models, Molecular | Enzyme Activation - drug effects | Glucokinase - metabolism | Benzamides - chemical synthesis | Drug Discovery | Enzyme Activators - chemical synthesis | Animals | Insulin-Secreting Cells - drug effects | Thiazoles - chemical synthesis | Diabetes Mellitus, Experimental - pathology | Thiazoles - chemistry | Mice | Thiazoles - pharmacology | Diabetes Mellitus, Type 2 - chemically induced | Diabetes Mellitus, Type 2 - pathology | Insulin-Secreting Cells - pathology | Diabetes Mellitus, Type 2 - drug therapy | Type 2 diabetes | Glucose | Isoenzymes | Glucose tolerance tests | Dextrose | Low density lipoproteins | Index Medicus
Journal Article
Journal Article
Biochemical Pharmacology, ISSN 0006-2952, 10/2019, Volume 168, pp. 149 - 161
Glucokinase (GK), a monomeric glucose-phosphorylating enzyme characterised by high structural flexibility, acts as a glucose sensor in pancreatic beta cells... 
Compound A | 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase | Protein-protein docking | RO-28-1675 | Glucokinase | Mannoheptulose | Pancreatic beta cells | Isoenzymes | Glutathione transferase | Diabetes | Glucose | Fructose | Dextrose | Protein binding | Blood proteins | Index Medicus
Journal Article
Diabetes, ISSN 0012-1797, 06/2019, Volume 68, Issue Supplement 1, p. 1151
Over the last two decades, many glucokinase activators (GKAs) advanced into clinical studies but failed to achieve proof of concept as antidiabetics until the... 
Glucokinase | Clinical trials | Homeostasis | Recovery of function | Glucose | Sensors | Hypoglycemia | Enzyme kinetics
Journal Article
Problemy Endokrinologii, ISSN 0375-9660, 2018, Volume 64, Issue 3, pp. 180 - 187
Journal Article
ANALYTICAL BIOCHEMISTRY, ISSN 0003-2697, 05/2015, Volume 477, pp. 62 - 68
Human hexokinase enzyme IV (EC 2.7.1.1) catalyzes the phosphorylation of glucose and regulates the level of glucose. This enzyme exhibits strong positive... 
Enzyme-activating assay | CHEMISTRY, ANALYTICAL | HOMEOSTASIS | F-19 spin signal | COMPETITION BINDING EXPERIMENTS | LIVER GLUCOKINASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | BIOCHEMICAL RESEARCH METHODS | TRANSITION | NMR | FLUORESCENCE | SPECTROSCOPY | Glucokinase | GLUCOSE | ALLOSTERIC ACTIVATORS | Ligands | DIABETES THERAPY
Journal Article
NATURE REVIEWS DRUG DISCOVERY, ISSN 1474-1776, 05/2009, Volume 8, Issue 5, pp. 351 - 351
Journal Article
The Lancet Diabetes & Endocrinology, ISSN 2213-8587, 09/2018, Volume 6, Issue 9, pp. 685 - 685
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 05/2017, Volume 27, Issue 9, pp. 2069 - 2073
Journal Article
Diabetes, Obesity and Metabolism, ISSN 1462-8902, 02/2016, Volume 18, Issue 2, pp. 191 - 195
Phase I studies have shown that AMG 151 activates glucokinase, a key enzyme in glucose homeostasis. The present randomized, placebo‐controlled phase IIa study... 
clinical trial | antidiabetic drug | glucokinase activator | type 2 diabetes | dose‐response relationship | Type 2 diabetes | Clinical trial | Antidiabetic drug | Glucokinase activator | Dose-response relationship | METFORMIN | THERAPY | ENDOCRINOLOGY & METABOLISM | dose-response relationship | Glycated Hemoglobin A - analysis | Hypoglycemia - epidemiology | Drugs, Investigational - adverse effects | Follow-Up Studies | Enzyme Activators - therapeutic use | Humans | Aminopyridines - adverse effects | Drugs, Investigational - therapeutic use | Incidence | Dose-Response Relationship, Drug | Hypoglycemia - prevention & control | Thiadiazoles - adverse effects | Aminopyridines - therapeutic use | Hypoglycemic Agents - administration & dosage | Enzyme Activators - administration & dosage | Thiadiazoles - therapeutic use | Postprandial Period | Adult | Hypoglycemia - chemically induced | Headache - chemically induced | Glucokinase - chemistry | Hypoglycemic Agents - therapeutic use | Aminopyridines - administration & dosage | Hyperglycemia - prevention & control | Blood Glucose - analysis | Double-Blind Method | Drug Administration Schedule | Glucokinase - metabolism | Diabetes Mellitus, Type 2 - blood | Hypertriglyceridemia - chemically induced | Hypertriglyceridemia - epidemiology | Headache - epidemiology | Enzyme Activators - adverse effects | Triglycerides - blood | Drugs, Investigational - administration & dosage | Least-Squares Analysis | Hyperglycemia - epidemiology | Diabetes Mellitus, Type 2 - drug therapy | Hypoglycemic Agents - adverse effects | Thiadiazoles - administration & dosage | Care and treatment | Fasting | Isoenzymes | Hypoglycemic agents | Glucose | Dextrose | Insulin | Diabetes | Index Medicus
Journal Article