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First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease.
TLDR
The synthesis, biological evaluation, and SAR of the small heterocyclic thiadiazolidinones (TDZD) are described as the first non-ATP competitive inhibitor of GSK-3beta, based on the reactivity of sulfenyl chlorides.
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GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS
TLDR
The variety of GSK-3 inhibitors are described with a specific emphasis on their biological activities in neurons and neurological disorders and the available data raise the hope that one or more of these drug design approaches will prove successful at stabilizing or reversing the aberrant neuropathology and cognitive deficits of certain central nervous system disorders.
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Glycogen Synthase Kinase-3
TLDR
This special issue is a timely “snapshot” of the current knowledge of GSK3 function in healthy and diseased brain, and highlights outstanding issues for future research on this important brain kinase.
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Preclinical efficacy on GSK‐3 inhibitors: Towards a future generation of powerful drugs
TLDR
Significant amounts of evidence have been accumulated showing preclinical efficacy for these new drugs, in very different models of several distinct pathologies, offering promising examples for new therapies for diabetes, cancer, inflammation, Alzheimer's disease and other neurological Pathologies, and mood disorders.
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Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.
TLDR
The search for the druggable sites on the enzyme using the fpocket algorithm allowed us to determine the binding sites of different GSK-3 ATP noncompetitive inhibitors, such as manzamine A and the new small molecule VP 0.7, providing evidence for potential allosteric inhibition of GK3.
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Guidelines for the use and interpretation of assays for monitoring autophagy (4th edition)1
TLDR
A set of guidelines for investigators to select and interpret methods to examine autophagy and related processes, and for reviewers to provide realistic and reasonable critiques of reports that are focused on these processes are presented.
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Glycogen synthase kinase 3 (GSK‐3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation
TLDR
This review is mainly focused on the new GSK‐3 inhibitors discovered or specifically developed for this enzyme, their chemical structure, synthesis, and structure–activity relationships, with the aim of providing some clues for the future optimization of these promising drugs.
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Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
TLDR
It is concluded that these dual AChE inhibitors are very promising disease-modifying agents for the treatment of Alzheimer's disease.
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Protein Kinase CK-1 Inhibitors As New Potential Drugs for Amyotrophic Lateral Sclerosis
TLDR
N-(benzothiazolyl)-2-phenyl-acetamides are valuable drug candidates for further studies and may be a new therapeutic approach for ALS and others pathologies in which TDP-43 is involved.
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Switching reversibility to irreversibility in glycogen synthase kinase 3 inhibitors: clues for specific design of new compounds.
TLDR
The results point out that these compounds might be useful pharmacological tools to explore physiological and pathological processes related to signaling pathways regulated by GSK-3 opening new avenues for the discovery of novel G SKS-3 inhibitors.
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