title: Benzothiazole derivatives augment glucose uptake in skeletal muscle cells and stimulate insulin secretion from pancreatic β-cells via AMPK activation.
abstract: Adenosine monophosphate-activated protein kinase (AMPK) has been identified as one of the major targets for antidiabetic drugs. This study describes two AMPK-activating agents 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole and 2-(propylthio)benzo[d]thiazol-6-ol, that increase the rate of glucose uptake in L6 myotubes and also augment glucose-stimulated insulin secretion in INS-1E β-cells and rat islets. We believe that such unique bi-functional compounds can be further used for the development of a new class of antidiabetic drugs.
authors.affiliation: Department of Pharmacology, Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, 91120, Jerusalem, Israel. shlomo.sasson@mail.huji.ac.il.
authors.forename: L
authors.initials: L
authors.lastname: Pasternak
authors.forename: E
authors.initials: E
authors.lastname: Meltzer-Mats
authors.forename: G
authors.initials: G
authors.lastname: Babai-Shani
authors.forename: G
authors.initials: G
authors.lastname: Cohen
authors.forename: O
authors.initials: O
authors.lastname: Viskind
authors.forename: J
authors.initials: J
authors.lastname: Eckel
authors.forename: E
authors.initials: E
authors.lastname: Cerasi
authors.forename: S
authors.initials: S
authors.lastname: Sasson
authors.forename: A
authors.initials: A
authors.lastname: Gruzman
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism*; D000818:Animals; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D004789:Enzyme Activation / Q000187:drug effects; D005947:Glucose / Q000378:metabolism*; D007328:Insulin / Q000378:metabolism*; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism*; D018482:Muscle, Skeletal / Q000166:cytology* / Q000187:drug effects; D051381:Rats
chemical_list: D052160:Benzothiazoles; D007328:Insulin; D055372:AMP-Activated Protein Kinases; D005947:Glucose