Beta-secretase inhibitors in phase I and phase II clinical trials for Alzheimer's disease

CEH Moussa - Expert opinion on investigational drugs, 2017 - Taylor & Francis
… clinical developments of BACE1 inhibitors and focuses on what is learned about these
inhibitors as a potential treatment. Expert opinion: BACE1 inhibition as a therapeutic strategy to …

Beta-secretase as a target for Alzheimer's disease drug discovery: an overview of in vitro methods for characterization of inhibitors

F Mancini, A De Simone, V Andrisano - Analytical and bioanalytical …, 2011 - Springer
… of selective non-peptide BACE1 inhibitors with a new chemical … inhibitors is crucial. This
review focuses on the description of the in vitro methods to test BACE1 activity and inhibition, …

Developing β‐secretase inhibitors for treatment of Alzheimer's disease

AK Ghosh, M Brindisi, J Tang - Journal of neurochemistry, 2012 - Wiley Online Library
… development of inhibitor drugs. During the past decade, steady progress has been made
in the evolution of β‐secretase inhibitors toward better drug properties. Recent inhibitors are …

Efficacy of Beta-Secretase-1 Enzyme Inhibitors in Alzheimer's Disease

R Yousefi, S Mokarmian, A Jamshidi - Journal of Advanced …, 2023 - journals.ekb.eg
… To prepare the molecular model of betasecretase enzyme, we removed the CNP520
inhibitor compound and water molecules from the model [PDB ID: 6EQM]. After preparing the …

β-secretase inhibitor; a promising novel therapeutic drug in Alzheimer's disease

KW Menting, JAHR Claassen - Frontiers in aging neuroscience, 2014 - frontiersin.org
inhibitors to bind at the active site, but inhibition generally occurs from an allosteric effect
where the inhibitor … • Non-competitive inhibition: binding of the inhibitor to the enzyme reduces …

Beta-secretase: structure, function, and evolution

C Venugopal, CM Demos… - CNS & Neurological …, 2008 - ingentaconnect.com
… BACE-1 cleavage is limiting for the production of Aβ, making it a particularly good drug
target for the generation of inhibitors that lower Aβ. A landmark discovery in AD was the …

In Silico Design of BetaSecretase Inhibitors in Alzheimer's Disease

EP Semighini - Chemical biology & drug design, 2015 - Wiley Online Library
… begins with the BACE ‐1 and which inhibition is considered one of the most promising
treatments … , and similarity search were used to design novel inhibitors of BACE ‐1, starting from …

Memapsin 2 (beta-secretase) inhibitors: drug development

AK Ghosh, N Kumaragurubaran, L Hong… - Current Alzheimer …, 2008 - ingentaconnect.com
… In vivo inhibition of Abeta production by memapsin 2 (betasecretase) inhibitors. J Neurochem
89: 1409-1416 (2004) [13] Chang WP, Downs D, Huang XP, Da H, Fung KM, and Tang, J. …

Results of beta secretase-inhibitor clinical trials support amyloid precursor protein-independent generation of beta amyloid in sporadic Alzheimer's disease

V Volloch, S Rits - Medical Sciences, 2018 - mdpi.com
The present review analyzes the results of recent clinical trials of β secretase inhibition in
sporadic Alzheimer’s disease (SAD), considers the striking dichotomy between successes in …

Human β-secretase (BACE) and BACE inhibitors

V John, JP Beck, MJ Bienkowski, S Sinha… - Journal of medicinal …, 2003 - ACS Publications
… in complexation with a variety of inhibitors has enabled great strides in development of new
classes of inhibitors, and a number of potent inhibitors of the enzyme have been reported. …