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Identification of Glycogen Synthase Kinase-3 Inhibitors with a Selective Sting for Glycogen Synthase Kinase-3α

Journal of Medicinal Chemistry, 2012
The glycogen synthase kinase-3 (GSK-3) has been linked to the pathogenesis of colorectal cancer, diabetes, cardiovascular disease, acute myeloid leukemia (AML), and Alzheimer's disease (AD). The debate on the respective contributions of GSK-3α and GSK-3β to AD pathology and AML is ongoing. Thus, the identification of potent GSK-3α-selective inhibitors,
Lo Monte F.   +14 more
openaire   +4 more sources

Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.

Journal of Medicinal Chemistry, 2012
Glycogen synthase kinase-3β, also called tau phosphorylating kinase, is a proline-directed serine/threonine kinase which was originally identified due to its role in glycogen metabolism.
S. Berg   +14 more
semanticscholar   +1 more source

Multisite phosphorylation of glycogen synthase

Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology, 1984
Glycogen synthase kinase-3 was isolated from rabbit skeletal muscle by an improved procedure. The purification was estimated to be 67000-fold and 0.2 mg of enzyme was isolated from 5000 g muscle, corresponding to an overall yield of 7%. The preparation was homogeneous by ultracentrifugal and electrophoretic criteria. The enzyme had a relative molecular
Woodgett, James R., Cohen, Philip
openaire   +4 more sources

glycogen synthase

Catalysis from A to Z, 2020
S. Reisse
semanticscholar   +1 more source

Inhibition of glycogen synthase kinase-3 by insulin mediated by protein kinase B

Nature, 1995
D. Cross   +4 more
semanticscholar   +1 more source

12 Liver Glycogen Synthase

1986
Publisher Summary This chapter reviews knowledge of mammalian liver glycogen synthase and its short-term regulation by covalent phosphorylation mechanisms. Elevated concentrations of insulin and glucose promote glycogen synthesis and the activation of glycogen synthase.
openaire   +2 more sources

Glycogen synthase in prenatal rat liver

Biochemical and Biophysical Research Communications, 1985
Glycogen synthase first appears in significant levels in fetal rat liver on day 18 of gestation (22 day term), but in a mostly inactive, phospho- form. This was reflected in a decreased affinity for its allosteric activator (increased A0.5 for glucose-6-phosphate), and with limited glycogen synthesis and accumulation.
openaire   +3 more sources

Structure and Regulation of Glycogen Synthase in the Brain

2019
Brain glycogen synthesis is a regulated, multi-step process that begins with glucose transport across the blood brain barrier and culminates with the actions of glycogen synthase and the glycogen branching enzyme to elongate glucose chains and introduce branch points in a growing glycogen molecule.
openaire   +3 more sources

Glycogen Synthase Kinase 3: A Kinase for All Pathways?

Current Topics in Developmental Biology, 2017
P. Patel, J. Woodgett
semanticscholar   +1 more source

Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.

European journal of medicinal chemistry, 2016
Mudasir Maqbool   +2 more
semanticscholar   +1 more source

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