Glycogen Synthase Kinase-3 (GSK3) Inhibition with Lithium in Combination with Tretinoin Induces Differentiation in Non-Promyelocytic Acute Myeloid Leukemia (AML)Lithium (Li) is a GSK3 inhibitor that induces differentiation and anti-proliferation of AML cells in vitro. Pre-clinical studies demonstrated ...
The chapter provides a short summary of the structure, substrate specificity, functions, and regulation of glycogen synthase kinase 3 protein. Glycogen synthase kinase 3 (GSK3) is a protein that phosphorylates and inhibits glycogen synthase, the enzyme that catalyzes the transfer of glucose from UDPG...
Glycogen synthase kinase (GSK3), a serine/threonine-protein kinase with two functionally distinct isoforms, α and β, was discovered in the context of glycogen metabolism and has emerged as a ubiquitous regulator of multiple signaling pathways19,20. Historically, GSK3β has been thought of as a...
Activation of canonical Wnt signaling by inhibition of glycogen synthase kinase 3 (GSK-3) has been shown to enhance bone mass, possibly by involving a number of mechanisms ranging from amplification of the mesenchymal stem cell pool to the commitment and differentiation of osteoblasts. Here we ...
The present invention relates to novel compounds for inhibiting glycogen synthase kinase-3 (GSK-3) and their use in regulating biological conditions mediated by GSK-3 activity and, more particularly, to the use of these compounds in the treatment of biological conditions such as type II diabetes,...
V. et al. 9-ING-41, a small-molecule glycogen synthase kinase-3 inhibitor, is active in neuroblastoma. Anti-cancer drugs 29, 717–724 (2018). CAS PubMed PubMed Central Google Scholar Wu, X. et al. Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma. Blood 134, ...
AR-A 014418 is a selective glycogen synthase kinase 3 (GSK-3) inhibitor (IC50 = 104 nM). Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices....
Polychronopouloset al(2004)Structural basis for the synthesis of indirubins as potent and selective inhibtors of glycogen synthase kinase-3 and cyclin dependent kinases.J.Med.Chem.47935 PMID: 14761195 Tsenget al(2006)The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.Chem.Bi...
GSK3β Inhibitor VIII is an ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC50 = 104 nM).{24857} It does not significantly inhibit the closely related cyclin-dependent kinase (Cdk)2 or Cdk5 (Kis = > 100 μM).{24857} GSK3β Inhib...
mechanismofglycogensynthase kinase313 (GSK一3B) inhibitor (2。 Z,3’E)一6一bromo—indirubin一3'-oxime(BIO)ondrugresistanceincoloncancercells. Methods:ThecoloncancerSW480andSW620cellsweretreatedwithBIO,5一fluorouraciI(5一Fu)andBIO/S—FU, separately.CelIcycledistribution,apoptosislevelande仟luxability...