1374671-64-3Relevant academic research and scientific papers
SMALL MOLECULE INHIBITORS OF SUPEROXIDE DISMUTASE EXPRESSION
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Paragraph 0091; 0092; 0093, (2015/08/04)
Disclosed are new small molecules and the uses thereof for inhibiting superoxide dismutase (SOD) expression. Also disclosed are pharmaceutical compositions comprising the small molecule inhibitors which may be administered in methods of treating diseases or disorders associated with elevated SOD expression or activity, including neurological diseases and disorders such as amyotrophic lateral sclerosis (ALS).
Identification of glycogen synthase kinase-3 inhibitors with a selective sting for glycogen synthase kinase-α
Lo Monte, Fabio,Kramer, Thomas,Gu, Jiamin,Anumala, Upendra Rao,Marinelli, Luciana,La Pietra, Valeria,Novellino, Ettore,Franco, Bénédicte,Demedts, David,Van Leuven, Fred,Fuertes, Ana,Dominguez, Juan Manuel,Plotkin, Batya,Eldar-Finkelman, Hagit,Schmidt, Boris
, p. 4407 - 4424 (2012/08/13)
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-α and GSK-3β to AD pathology and AML is ongoing. Thus, the identification of potent GSK-α-selective inhibitors, endowed with favorable pharmacokinetic properties, may elucidate the effect of GSK-α inhibition in AD and AML models. The analysis of all available crystallized GSK-3 structures provided a simplified scheme of the relevant hot spots responsible for ligand binding and potency. This resulted in the identification of novel scorpion shaped GSK-3 inhibitors. It is noteworthy, compounds 14d and 15b showed the highest GSK-α selectivity reported so far. In addition, compound 14d did not display significant inhibition of 48 out of 50 kinases in the test panel. The GSK-3 inhibitors were further profiled for efficacy and toxicity in the wild-type (wt) zebrafish embryo assay.
