Literature DB >> 15588077

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Shawn J Stachel1, Craig A Coburn, Thomas G Steele, Kristen G Jones, Elizabeth F Loutzenhiser, Alison R Gregro, Hemaka A Rajapakse, Ming-Tain Lai, Ming-Chih Crouthamel, Min Xu, Katherine Tugusheva, Janet E Lineberger, Beth L Pietrak, Amy S Espeseth, Xiao-Ping Shi, Elizabeth Chen-Dodson, M Katharine Holloway, Sanjeev Munshi, Adam J Simon, Lawrence Kuo, Joseph P Vacca.   

Abstract

We describe the development of cell-permeable beta-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50 < 100 nM), these inhibitors display impressive selectivity against other biologically relevant aspartyl proteases.

Entities:  

Mesh：

Substances：

Year:  2004        PMID： 15588077     DOI： 10.1021/jm049379g

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  73 in total

1.  The neural cell adhesion molecules L1 and CHL1 are cleaved by BACE1 protease in vivo.

Authors:  Lujia Zhou; Soraia Barão; Mathias Laga; Katrijn Bockstael; Marianne Borgers; Harry Gijsen; Wim Annaert; Diederik Moechars; Marc Mercken; Kris Gevaert; Kris Gevaer; Bart De Strooper
Journal:  J Biol Chem       Date:  2012-06-12       Impact factor: 5.157

2.  Secretome protein enrichment identifies physiological BACE1 protease substrates in neurons.

Authors:  Peer-Hendrik Kuhn; Katarzyna Koroniak; Sebastian Hogl; Alessio Colombo; Ulrike Zeitschel; Michael Willem; Christiane Volbracht; Ute Schepers; Axel Imhof; Albrecht Hoffmeister; Christian Haass; Steffen Roßner; Stefan Bräse; Stefan F Lichtenthaler
Journal:  EMBO J       Date:  2012-06-22       Impact factor: 11.598

3.  Isoflavonoids from Ficus benjamina and their inhibitory activity on BACE1.

Authors:  Jingqiu Dai; Dai Shen; Wesley Y Yoshida; Stephen M Parrish; Philip G Williams
Journal:  Planta Med       Date:  2012-07-04       Impact factor: 3.352

4.  ADAM10 is the physiologically relevant, constitutive alpha-secretase of the amyloid precursor protein in primary neurons.

Authors:  Peer-Hendrik Kuhn; Huanhuan Wang; Bastian Dislich; Alessio Colombo; Ulrike Zeitschel; Joachim W Ellwart; Elisabeth Kremmer; Steffen Rossner; Stefan F Lichtenthaler
Journal:  EMBO J       Date:  2010-07-30       Impact factor: 11.598

5.  The novel membrane protein TMEM59 modulates complex glycosylation, cell surface expression, and secretion of the amyloid precursor protein.

Authors:  Sylvia Ullrich; Anna Münch; Stephanie Neumann; Elisabeth Kremmer; Jörg Tatzelt; Stefan F Lichtenthaler
Journal:  J Biol Chem       Date:  2010-04-28       Impact factor: 5.157

6.  Inhibition of beta-secretase in vivo via antibody binding to unique loops (D and F) of BACE1.

Authors:  Lujia Zhou; Lucia Chávez-Gutiérrez; Katrijn Bockstael; Ragna Sannerud; Wim Annaert; Patrick C May; Eric Karran; Bart De Strooper
Journal:  J Biol Chem       Date:  2011-01-05       Impact factor: 5.157

7.  Full-length cellular β-secretase has a trimeric subunit stoichiometry, and its sulfur-rich transmembrane interaction site modulates cytosolic copper compartmentalization.

Authors:  Filip Liebsch; Mark R P Aurousseau; Tobias Bethge; Hugo McGuire; Silvia Scolari; Andreas Herrmann; Rikard Blunck; Derek Bowie; Gerd Multhaup
Journal:  J Biol Chem       Date:  2017-06-21       Impact factor: 5.157

Review 8.  The development of anti-amyloid therapy for Alzheimer's disease : from secretase modulators to polymerisation inhibitors.

Authors:  Paul S Aisen
Journal:  CNS Drugs       Date:  2005       Impact factor: 5.749

9.  Reduced BACE1 activity enhances clearance of myelin debris and regeneration of axons in the injured peripheral nervous system.

Authors:  Mohamed H Farah; Bao Han Pan; Paul N Hoffman; Dana Ferraris; Takashi Tsukamoto; Thien Nguyen; Philip C Wong; Donald L Price; Barbara S Slusher; John W Griffin
Journal:  J Neurosci       Date:  2011-04-13       Impact factor: 6.167

10.  Transcriptional regulation of beta-secretase by p25/cdk5 leads to enhanced amyloidogenic processing.

Authors:  Yi Wen; W Haung Yu; Bryan Maloney; Jason Bailey; Junrong Ma; Isabelle Marié; Thomas Maurin; Lili Wang; Helen Figueroa; Mathieu Herman; Pavan Krishnamurthy; Li Liu; Emmanuel Planel; Lit-Fui Lau; Debomoy K Lahiri; Karen Duff
Journal:  Neuron       Date:  2008-03-13       Impact factor: 17.173
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.