Literature DB >> 27020305

Part 2. Notch-sparing γ-secretase inhibitors: The study of novel γ-amino naphthyl alcohols.

Han-Xun Wei1, Dai Lu1, Vivien Sun1, Jing Zhang1, Yongli Gu1, Pamela Osenkowski1, Wenjuan Ye1, Dennis J Selkoe1, Michael S Wolfe1, Corinne E Augelli-Szafran2.   

Abstract

One therapeutic approach for Alzheimer's disease is to inhibit the cleavage of the amyloid precursor protein (APP) by γ-secretase. At the beginning of a series of studies from our laboratories, a series of novel γ-amino alcohols (1) were found to possess γ-secretase inhibitory activity and Notch-sparing effects. A new one-pot synthesis of γ-amino alcohols and the structure-activity relationship (SAR) of these analogs will be discussed.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Alzheimer’s disease; Aβ production; Notch-processing; γ-Amino alcohols; γ-Secretase inhibitors

Mesh:

Substances:

Year:  2016        PMID: 27020305      PMCID: PMC8323768          DOI: 10.1016/j.bmcl.2016.03.042

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  10 in total

1.  Activity-dependent isolation of the presenilin- gamma -secretase complex reveals nicastrin and a gamma substrate.

Authors:  William P Esler; W Taylor Kimberly; Beth L Ostaszewski; Wenjuan Ye; Thekla S Diehl; Dennis J Selkoe; Michael S Wolfe
Journal:  Proc Natl Acad Sci U S A       Date:  2002-02-26       Impact factor: 11.205

Review 2.  γ-secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopes.

Authors:  Bruno P Imbimbo; Giuseppe A M Giardina
Journal:  Curr Top Med Chem       Date:  2011       Impact factor: 3.295

3.  Notch and the amyloid precursor protein are cleaved by similar gamma-secretase(s).

Authors:  W Taylor Kimberly; William P Esler; Wenjuan Ye; Beth L Ostaszewski; Jun Gao; Thekla Diehl; Dennis J Selkoe; Michael S Wolfe
Journal:  Biochemistry       Date:  2003-01-14       Impact factor: 3.162

Review 4.  Alzheimer's disease: clinical trials and drug development.

Authors:  Francesca Mangialasche; Alina Solomon; Bengt Winblad; Patrizia Mecocci; Miia Kivipelto
Journal:  Lancet Neurol       Date:  2010-07       Impact factor: 44.182

5.  gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site.

Authors:  Patrick C Fraering; Wenjuan Ye; Matthew J LaVoie; Beth L Ostaszewski; Dennis J Selkoe; Michael S Wolfe
Journal:  J Biol Chem       Date:  2005-10-19       Impact factor: 5.157

Review 6.  gamma-Secretase in biology and medicine.

Authors:  Michael S Wolfe
Journal:  Semin Cell Dev Biol       Date:  2008-12-31       Impact factor: 7.727

Review 7.  Alzheimer's disease: genotypes, phenotypes, and treatments.

Authors:  D J Selkoe
Journal:  Science       Date:  1997-01-31       Impact factor: 47.728

8.  Purification and characterization of the human gamma-secretase complex.

Authors:  Patrick C Fraering; Wenjuan Ye; Jean-Marc Strub; Georgia Dolios; Matthew J LaVoie; Beth L Ostaszewski; Alain van Dorsselaer; Rong Wang; Dennis J Selkoe; Michael S Wolfe
Journal:  Biochemistry       Date:  2004-08-03       Impact factor: 3.162

9.  Presenilin 1 regulates the processing of beta-amyloid precursor protein C-terminal fragments and the generation of amyloid beta-protein in endoplasmic reticulum and Golgi.

Authors:  W Xia; J Zhang; B L Ostaszewski; W T Kimberly; P Seubert; E H Koo; J Shen; D J Selkoe
Journal:  Biochemistry       Date:  1998-11-24       Impact factor: 3.162

Review 10.  Inhibition and modulation of gamma-secretase for Alzheimer's disease.

Authors:  Michael S Wolfe
Journal:  Neurotherapeutics       Date:  2008-07       Impact factor: 7.620

  10 in total
  1 in total

1.  Anticancer activities of a β-amino alcohol ligand and nanoparticles of its copper(ii) and zinc(ii) complexes evaluated by experimental and theoretical methods.

Authors:  Zahra Mardani; Reza Kazemshoar-Duzduzani; Keyvan Moeini; Alireza Hajabbas-Farshchi; Cameron Carpenter-Warren; Alexandra M Z Slawin; J Derek Woollins
Journal:  RSC Adv       Date:  2018-08-13       Impact factor: 4.036

  1 in total

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