Small molecule glucokinase activators disturb lipid homeostasis and induce fatty liver in rodents: A warning for therapeutic applications in humans

British Journal of Pharmacology

Volumn 168, Issue 2, 2013, Pages 339-353

  De Ceuninck, Frédéric ^a   Kargar, Catherine ^a   Ilic, Catherine ^a   Caliez, Audrey ^a   Rolin, Jean Olivier ^a   Umbdenstock, Thierry ^b   Vinson, Cédric ^b   Combettes, Murielle ^a   De Fanti, Brant ^a   Harley, Elizabeth ^a   Sadlo, Marjorie ^a   Lefèvre, Anne Laure ^a   Broux, Olivier ^a   Wierzbicki, Michel ^a   Fourquez, Jean Marie ^a   Perron Sierra, Françoise ^a   Kotschy, András ^c   Ktorza, Alain ^a  

^a INSTITUT DE RECHERCHES SERVIER   (France)

^b INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

^c Servier Research Institute of Medicinal Chemistry   (Hungary)

Author keywords

adverse outcome; diabetes; fatty liver; glucokinase; glucose homeostasis; hepatic steatosis; lipids; rodents; triglycerides

Indexed keywords

ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; ANTIDIABETIC AGENT; ASPARTATE AMINOTRANSFERASE; FATTY ACID; GKA 50; GLUCOKINASE ACTIVATOR; GLUCOSE; HEMOGLOBIN A1C; N 00234379; N 00236460; N 00255785; N 00259193; N 00263726; N 00263996; N 00268746; OLEIC ACID; PIRAGLIATIN; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ALKALINE PHOSPHATASE BLOOD LEVEL; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDIABETIC ACTIVITY; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; CONTROLLED STUDY; DIABETES MELLITUS; DRUG ABSORPTION; DRUG DOSE INCREASE; DRUG EFFECT; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; FATTY LIVER; GLUCOSE BLOOD LEVEL; GLYCOGEN SYNTHESIS; HYPERGLYCEMIA; IN VIVO STUDY; INSULIN RELEASE; LIPID METABOLISM; LIVER CELL; LOW DRUG DOSE; NONHUMAN; OUTCOME ASSESSMENT; PRIORITY JOURNAL; RAT; REVIEW; RISK FACTOR; TISSUE LEVEL; TRIACYLGLYCEROL BLOOD LEVEL;

ANIMALS; BLOOD GLUCOSE; CACO-2 CELLS; CELL LINE, TUMOR; CELLS, CULTURED; DIABETES MELLITUS, TYPE 2; ENZYME ACTIVATORS; FATTY LIVER; GLUCOKINASE; HEMOGLOBIN A, GLYCOSYLATED; HEPATOCYTES; HOMEOSTASIS; HUMANS; HYPOGLYCEMIC AGENTS; INTESTINAL ABSORPTION; LIPID METABOLISM; MALE; MICE; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; RATS, ZUCKER;

EID: 84871604441     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.02184.x     Document Type: Review

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