1333227-64-7Relevant academic research and scientific papers
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis
Charton, Julie,Gauriot, Marion,Guo, Qing,Hennuyer, Nathalie,Marechal, Xavier,Dumont, Julie,Hamdane, Malika,Pottiez, Virginie,Landry, Valerie,Sperandio, Olivier,Flipo, Marion,Buee, Luc,Staels, Bart,Leroux, Florence,Tang, Wei-Jen,Deprez, Benoit,Deprez-Poulain, Rebecca
, p. 184 - 193 (2014/05/06)
Insulin degrading enzyme (IDE) is a highly conserved zinc metalloprotease that is involved in the clearance of various physiologically peptides like amyloid-beta and insulin. This enzyme has been involved in the physiopathology of diabetes and Alzheimer's disease. We describe here a series of small molecules discovered by screening. Co-crystallization of the compounds with IDE revealed a binding both at the permanent exosite and at the discontinuous, conformational catalytic site. Preliminary structure-activity relationships are described. Selective inhibition of amyloid-beta degradation over insulin hydrolysis was possible. Neuroblastoma cells treated with the optimized compound display a dose-dependent increase in amyloid-beta levels.
Ligands of insulin degrading enzyme and their uses
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Page/Page column, (2013/03/26)
The invention relates to ligands of insulin degrading enzyme and to their uses. The ligands of the invention are non peptidic and bind specifically to the exosite of insulin degrading enzyme. They are useful, in particular a use in the pharmaceutical field.
