Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates-Reference-Cited by-同舟云学术

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

Published:2016-03-22 Issue:7 Volume:59 Page:3231-3248
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Mandal Mihirbaran¹,Wu Yusheng¹,Misiaszek Jeffrey¹,Li Guoqing¹,Buevich Alexei¹,Caldwell John P.¹,Liu Xiaoxiang¹,Mazzola Robert D.¹,Orth Peter¹,Strickland Corey¹,Voigt Johannes¹,Wang Hongwu¹,Zhu Zhaoning¹,Chen Xia¹,Grzelak Michael¹,Hyde Lynn A.¹,Kuvelkar Reshma¹,Leach Prescott T.¹,Terracina Giuseppe¹,Zhang Lili¹,Zhang Qi¹,Michener Maria S.¹,Smith Brad¹,Cox Kathleen¹,Grotz Diane¹,Favreau Leonard¹,Mitra Kaushik¹,Kazakevich Irina¹,McKittrick Brian A.¹,Greenlee William¹,Kennedy Matthew E.¹,Parker Eric M.¹,Cumming Jared N.¹,Stamford Andrew W.¹

Affiliation:

1. Department of Global Chemistry, ‡Department of Neuroscience, §Department of Safety Assessment and Laboratory Animal Research, ∥Department of Discovery Pharmaceutical Sciences, and ⊥Department of Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States

Funder

Basic Energy Sciences

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.5b01995

Reference72 articles.

1. Alzheimer’s Disease Facts and Figures;Alzheimer’s Association:Chicago, 2015; http://www.alz.org/facts/downloads/facts_figures_2015.pdf(accessed February 13, 2016).

2. World Alzheimer Report;Alzheimer’s Disease International:London, 2015, http://www.alz.co.uk/research/WorldAlzheimerReport2015.pdf(accessed February 13, 2016).

3. Current Treatment for Alzheimer Disease and Future Prospects

4. Mechanisms Behind the Neuroprotective Actions of Cholinesterase Inhibitors in Alzheimer Disease

5. Efficacy and Safety of Memantine in Moderate-to-Severe Alzheimer Disease: The Evidence to Date

Cited by 37 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Identification Mechanism of BACE1 on Inhibitors Probed by Using Multiple Separate Molecular Dynamics Simulations and Comparative Calculations of Binding Free Energies;Molecules;2023-06-15

2. Discovery of SYD5115, a novel orally active small molecule TSH-R antagonist;Bioorganic & Medicinal Chemistry;2023-04

3. The Alzheimer’s disease-linked protease BACE1 modulates neuronal IL-6 signaling through shedding of the receptor gp130;Molecular Neurodegeneration;2023-02-21

4. Drug Discovery to Drug Development of BACE1 Inhibitor as Antialzheimer’s: A Review;Current Topics in Medicinal Chemistry;2023-01

5. Guanidine-based β amyloid precursor protein cleavage enzyme 1 (BACE-1) inhibitors for the Alzheimer's disease (AD): A review;Bioorganic & Medicinal Chemistry;2022-11