Currently, nirogacestat (Ogsiveo) is the first and only formulation available in the gamma secretase inhibitor class. The drug received Fast Track, Breakthrough Therapy and Orphan designation from the FDA and was finally approved by the FDA in November 2023. How are gamma secretase inhibitors us...
A Gamma Secretase Inhibitor is a compound that can modulate the activity of the protease complex called gamma-secretase, which is involved in the production of amyloid beta (Aβ) without completely inhibiting its function. These inhibitors are preferred as they can reduce Aβ production without dis...
Gamma-secretase inhibitor such as DAPT, reduces the CSCs by inhibiting Notch pathway. Apart from its advantages, DAPT causes side effects which making it necessary to use new strategies. Since vitamin C (Ascorbic Acid: AA) receptors are high on CSCs, they are high in AA uptake and can be ...
Thein S, Shiovitz T, Pilcher G, Colby S, Rollin L, Dockens R, Pachai C, Portelius E, Andreasson U, Blennow K, Soares H, Albright C, Feldman HH, Berman RM: Safety and tolerability of the gamma-secretase inhibitor avagacestat in a phase 2 study of mild to moderate Alzheimer disease....
et al., “Adipsin, a Biomarker of Gastrointestinal Toxicity Mediated by a Functional γ-Secretase inhibitor”, The J. of Biological Chemistry, vol. 278(46), pp. 46107-46116 (2003). Struhl, G. et al., “Requirements for Presenilin-Dependent Cleavage of Notch and Other ransmembrane Proteins...
It has been postulated that APP substrate selective inhibitors of gamma-secretase would be preferable to non-selective inhibitors from a safety perspective for AD therapy. Methods In vitro assays monitoring inhibitor potencies at APP γ-site cleavage (equivalent to Aβ40), and Notch ε-site ...
Signaling PathwaysNeuroscience-Stem CellsBeta Amyloid-Gamma-secretaseMDR-1339 TOPRelated productsBioactivityChemical infoStorage&SolubilityCalculatorMDR-1339 Catalog No. TQ0026Cas No. 1018946-38-7 Alias DWK-1339 MDR-1339 (DWK-1339) is an orally active, blood-brain-barrier-permeable inhibitor of amyloid...
(α, γ, δ) at 10 µM increased the production and decreased the degradation of Aβ in SH-SY5Y over expressing wild type APP by increasing the protein expression of β- and γ-secretase enzyme. However, their results showed that ATF had only minor effects on Aβ production whereas ...
The present disclosure relates to methods of using antibody conjugates with binding specificity for BCMA (BCMA) and its isoforms and homologs in combination with a gamma secretase i
or an inhibitor of gamma-secretase, b) administering a test compound to said system, and incubating said system in gamma-secretase complex-destabilizing conditions, and c) quantification of the binding interaction between said gamma-secretase complex and said substrate-like interactor in said system,...