- |||||||||| DEVELOPING BETA-SECRETASE INHIBITORS FOR TREATMENT OF ALZHEIMER’S DISEASE () - Mar 9, 2022 - Abstract #ADPD2022ADPD_1122;
The capability of BACE1 to apply such a therapeutic candidate for AD therapy has just been examined during the previous decade. There is proof indicate that the 1 inhibitor administrating time is critical and make big difference in how successful they are in curing AD.
- |||||||||| mecripyrine (Y-1) / Simcere, Yantai YenePharma, LY-2811376 / Eli Lilly
Journal: Unprecedented polycyclic polyprenylated acylphloroglucinols with anti-Alzheimer's activity from St. John's wort. (Pubmed Central) - Sep 28, 2021
Furthermore, compound 6 showed better therapeutic effects with respect to the reduction of pathological and cognitive impairments in 3 × Tg AD mice than LY2811376. Compound 6 represents the first multitargeted natural product that could activate PP2A and simultaneously inhibit BACE1, which highlights compound 6 as a promising lead compound and a versatile scaffold in AD drug development.
- |||||||||| Review, Journal: Selective Secretase Targeting for Alzheimer's Disease Therapy. (Pubmed Central) - Sep 17, 2021
Such therapeutic tools shall focus on slowing down or minimizing the progression of neuronal damage. Here, we summarize structures and the activities of the latest compounds designed for AD treatment, with remarkable in vitro, in vivo, and clinical phase activities.
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Clinical, Journal: Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor. (Pubmed Central) - Aug 25, 2021
LY2886721 advanced to Phase II, but development was halted due to abnormally elevated liver enzymes. Herein, we report the discovery and clinical development of LY3202626, a highly potent, CNS-penetrant, and low-dose BACE inhibitor, which successfully addressed these key development challenges.
- |||||||||| LY-2811376 / Eli Lilly
Journal: Near-infrared Fluorescence Ocular Imaging (NIRFOI) of Alzheimer's Disease. (Pubmed Central) - Aug 1, 2019
Compared to fluorescence microscopic imaging, NIRFOI captures signals with a wide angle (large field of view (FOV)) and can be used to detect soluble Aβs. We believe that NIRFOI has remarkable translational potential for future human studies and can be a potential imaging technology for fast, cheap, accessible, and reliable screening of AD in the future.
- |||||||||| LY-2811376 / Eli Lilly
Journal: Conformational dynamics of cathepsin D and binding to a small-molecule BACE1 inhibitor. (Pubmed Central) - May 18, 2019
We believe that NIRFOI has remarkable translational potential for future human studies and can be a potential imaging technology for fast, cheap, accessible, and reliable screening of AD in the future. ...Finally, we investigate binding of the inhibitor LY2811376 developed by Eli Lilly to BACE1 and CatD...This work highlights the complexity and challenge in structure-based drug design where receptor-ligand binding induces protonation state change in both the protein and the inhibitor.
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