Predicting memapsin 2 (β-secretase) hydrolytic activity
نویسندگان
چکیده
منابع مشابه
Amyloid-beta reduction by memapsin 2 (beta-secretase) immunization.
Memapsin 2 (beta-secretase, BACE1) is the protease that initiates cleavage of beta-amyloid precursor protein leading to the production of amyloid-beta (Abeta) and the onset of Alzheimer's disease (AD). Reducing Abeta by targeting memapsin 2 is a major strategy in developing new AD therapy. Here, in a proof-of-concept study, we show that immunization of transgenic AD mice (Tg2576) with memapsin ...
متن کاملDesign of Potent and Highly Selective Inhibitors for Human β-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes.
Design, synthesis and evaluation of very potent and selective β-Secretase 2 (memapsin 1, BACE 2) inhibitors are described. The inhibitors were designed specifically to interact with the S2'-site of β-secretase 2 to provide >170,000-fold selectivity over β-secretase (BACE 1) and >15,000-fold selectivity over cathepsin D. BACE 2 is implicated in Type 2 diabetes. The studies serve as an important ...
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Giuseppina Tesco,* Young Ho Koh, Eugene L. Kang, Andrew N. Cameron, Shinjita Das, Miguel Sena-Esteves, Mikko Hiltunen, Shao-Hua Yang, Zhenyu Zhong, Yong Shen, James W. Simpkins, and Rudolph E. Tanzi* Genetics and Aging Research Unit Neuroscience Center Massachusetts General Hospital, Charlestown, MA 02129, USA Department of Pharmacology and Neuroscience, University of North Texas Health Science...
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Accumulation and deposition of amyloid-β peptide (Aβ) in the brain is a primary cause of the pathogenesis of Alzheimer's disease (AD). Aβ is generated from amyloid-β precursor protein (APP) through sequential cleavages first by β-secretase and then by γ-secretase. Inhibiting β-secretase activity is believed to be one of the most promising strategies for AD treatment. In the present study, we fo...
متن کاملMemapsin 2, a drug target for Alzheimer's disease.
Mempasin 2, a beta-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of beta-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been esta...
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ژورنال
عنوان ژورنال: Protein Science
سال: 2010
ISSN: 0961-8368
DOI: 10.1002/pro.502