Literature DB >> 20817005

BACE: Therapeutic target and potential biomarker for Alzheimer's disease.

Geneviève Evin1, Adel Barakat, Colin L Masters.   

Abstract

β-Site APP-cleaving enzyme (BACE) is a membrane-bound aspartyl protease involved in the production of Alzheimer's disease (AD) Aβ amyloid peptides. This enzyme is ubiquitously expressed, with highest levels in the brain and pancreas. Its cellular trafficking is tightly controlled as it recycles between endosomes and trans-Golgi network. BACE expression increases in response to aging and various stress stimuli. It is elevated in the brain cortex of AD sufferers, and increased levels of BACE in the cerebrospinal fluid of patients with mild cognitive impairment may provide an early biomarker of AD. BACE is considered as a rational drug target for AD therapy, and inhibitors are under development. Anomalies in the behaviour and biochemistry of BACE(-/-) mice have pointed to the role this enzyme plays in the processing of neuregulin and of voltage-gated sodium channel β-subunit. A full understanding of BACE biology in health and disease is needed to establish a safe AD therapy based on BACE inhibitors.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20817005     DOI: 10.1016/j.biocel.2010.08.017

Source DB:  PubMed          Journal:  Int J Biochem Cell Biol        ISSN: 1357-2725            Impact factor:   5.085


  27 in total

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Review 2.  Cellular Trafficking of Amyloid Precursor Protein in Amyloidogenesis Physiological and Pathological Significance.

Authors:  Noralyn Basco Mañucat-Tan; Khalil Saadipour; Yan-Jiang Wang; Larisa Bobrovskaya; Xin-Fu Zhou
Journal:  Mol Neurobiol       Date:  2018-05-24       Impact factor: 5.590

3.  Autophagy-mediated Regulation of BACE1 Protein Trafficking and Degradation.

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Journal:  J Biol Chem       Date:  2016-12-27       Impact factor: 5.157

4.  Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.

Authors:  Arun K Ghosh; Margherita Brindisi; Yu-Chen Yen; Emilio L Cárdenas; Jean-Rene Ella-Menye; Nagaswamy Kumaragurubaran; Xiangping Huang; Jordan Tang; Andrew D Mesecar
Journal:  Bioorg Med Chem Lett       Date:  2017-04-08       Impact factor: 2.823

5.  Stimulus-Responsive Prochelators for Manipulating Cellular Metals.

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6.  Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators.

Authors:  Kevin D Rynearson; Ronald N Buckle; R Jason Herr; Nicholas J Mayhew; Xinchao Chen; William D Paquette; Samuel A Sakwa; Jinhai Yang; Keith D Barnes; Phuong Nguyen; William C Mobley; Graham Johnson; Juinn H Lin; Rudolph E Tanzi; Steven L Wagner
Journal:  Bioorg Med Chem       Date:  2020-09-01       Impact factor: 3.641

7.  Monitoring β-secretase activity in living cells with a membrane-anchored FRET probe.

Authors:  Drew S Folk; Justin C Torosian; Sunhee Hwang; Dewey G McCafferty; Katherine J Franz
Journal:  Angew Chem Int Ed Engl       Date:  2012-09-28       Impact factor: 15.336

Review 8.  Voltage-gated sodium channel β subunits: The power outside the pore in brain development and disease.

Authors:  Jacob M Hull; Lori L Isom
Journal:  Neuropharmacology       Date:  2017-09-18       Impact factor: 5.250

9.  Structure-based design, synthesis and biological evaluation of novel β-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.

Authors:  Arun K Ghosh; Margherita Brindisi; Yu-Chen Yen; Xiaoming Xu; Xiangping Huang; Thippeswamy Devasamudram; Geoffrey Bilcer; Hui Lei; Gerald Koelsch; Andrew D Mesecar; Jordan Tang
Journal:  Bioorg Med Chem Lett       Date:  2014-12-06       Impact factor: 2.823

10.  Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease.

Authors:  Fredrik Jeppsson; Susanna Eketjäll; Juliette Janson; Sofia Karlström; Susanne Gustavsson; Lise-Lotte Olsson; Ann-Cathrine Radesäter; Bart Ploeger; Gvido Cebers; Karin Kolmodin; Britt-Marie Swahn; Stefan von Berg; Tjerk Bueters; Johanna Fälting
Journal:  J Biol Chem       Date:  2012-10-09       Impact factor: 5.157

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