Literature DB >> 22860177

ACS chemical neuroscience molecule spotlight on Begacestat (GSI-953).

Corey R Hopkins1.   

Abstract

A "second generation" γ-secretase, Begacestat (GSI-953), which is more selective against Notch-signaling, has shown promise in recent Phase I clinical trials. Begacestat, a novel, 2,5-disubsitituted thiophene sulfonamide from Wyeth (now Pfizer) is under evaluation for the treatment of Alzheimer's disease.

Entities:  

Keywords:  Alzheimer's disease, γ-secretase inhibitors, GSI, Aβ-peptides

Mesh：

Substances：

Year:  2012        PMID： 22860177      PMCID： PMC3369785          DOI： 10.1021/cn200124u

Source DB:  PubMed          Journal:  ACS Chem Neurosci        ISSN： 1948-7193            Impact factor:   4.418


  9 in total

Review 1.  ACS chemical neuroscience molecule spotlight on ELND006: another γ-secretase inhibitor fails in the clinic.

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2011-06-15       Impact factor: 4.418

2.  ACS chemical neuroscience molecule spotlight on semagacestat (LY450139).

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2010-08-18       Impact factor: 4.418

Review 3.  Alzheimer's disease: the amyloid cascade hypothesis.

Authors:  J A Hardy; G A Higgins
Journal:  Science       Date:  1992-04-10       Impact factor: 47.728

Review 4.  The molecular pathology of Alzheimer's disease.

Authors:  D J Selkoe
Journal:  Neuron       Date:  1991-04       Impact factor: 17.173

5.  Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.

Authors:  Anthony Kreft; Boyd Harrison; Suzan Aschmies; Kevin Atchison; David Casebier; Derek C Cole; George Diamantidis; John Ellingboe; Diane Hauze; Yun Hu; Donna Huryn; Mei Jin; Dennis Kubrak; Peimin Lu; Joseph Lundquist; Charles Mann; Robert Martone; William Moore; Aram Oganesian; Alex Porte; Dave R Riddell; June Sonnenberg-Reines; Joseph R Stock; Shaiu-Ching Sun; Erik Wagner; Kevin Woller; Zheng Xu; Hua Zhou; J Steven Jacobsen
Journal:  Bioorg Med Chem Lett       Date:  2008-05-20       Impact factor: 2.823

Review 6.  The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics.

Authors:  John Hardy; Dennis J Selkoe
Journal:  Science       Date:  2002-07-19       Impact factor: 47.728

7.  (S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.

Authors:  Derek C Cole; Joseph R Stock; Anthony F Kreft; Madelene Antane; Suzan H Aschmies; Kevin P Atchison; David S Casebier; Thomas A Comery; George Diamantidis; John W Ellingboe; Boyd L Harrison; Yun Hu; Mei Jin; Dennis M Kubrak; Peimin Lu; Charles W Mann; Robert L Martone; William J Moore; Aram Oganesian; David R Riddell; June Sonnenberg-Reines; Shaiu-Ching Sun; Erik Wagner; Zheng Wang; Kevin R Woller; Zheng Xu; Hua Zhou; J Steven Jacobsen
Journal:  Bioorg Med Chem Lett       Date:  2008-12-06       Impact factor: 2.823

8.  Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

Authors:  Scott C Mayer; Anthony F Kreft; Boyd Harrison; Magid Abou-Gharbia; Madelene Antane; Suzan Aschmies; Kevin Atchison; Michael Chlenov; Derek C Cole; Thomas Comery; George Diamantidis; John Ellingboe; Kristi Fan; Rocco Galante; Cathleen Gonzales; Douglas M Ho; Molly E Hoke; Yun Hu; Donna Huryn; Uday Jain; Mei Jin; Kenneth Kremer; Dennis Kubrak; Melissa Lin; Peimin Lu; Ron Magolda; Robert Martone; William Moore; Aram Oganesian; Menelas N Pangalos; Alex Porte; Peter Reinhart; Lynn Resnick; David R Riddell; June Sonnenberg-Reines; Joseph R Stock; Shaiu-Ching Sun; Erik Wagner; Ting Wang; Kevin Woller; Zheng Xu; Margaret M Zaleska; Joseph Zeldis; Minsheng Zhang; Hua Zhou; J Steven Jacobsen
Journal:  J Med Chem       Date:  2008-12-11       Impact factor: 7.446

9.  Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Authors:  Robert L Martone; Hua Zhou; Kevin Atchison; Thomas Comery; Jane Z Xu; Xinyi Huang; Xioahai Gong; Mei Jin; Anthony Kreft; Boyd Harrison; Scott C Mayer; Suzan Aschmies; Cathleen Gonzales; Margaret M Zaleska; David R Riddell; Erik Wagner; Peimin Lu; Shaiu-Ching Sun; June Sonnenberg-Reines; Aram Oganesian; Karissa Adkins; Michael W Leach; David W Clarke; Donna Huryn; Magid Abou-Gharbia; Ronald Magolda; Jonathan Bard; Glen Frick; Sangeeta Raje; S Bradley Forlow; Carrie Balliet; Michael E Burczynski; Peter H Reinhart; Hong I Wan; Menelas N Pangalos; J Steven Jacobsen
Journal:  J Pharmacol Exp Ther       Date:  2009-08-11       Impact factor: 4.030
  9 in total
  5 in total

1.  Quantitative Measurement of γ-Secretase-mediated Amyloid Precursor Protein and Notch Cleavage in Cell-based Luciferase Reporter Assay Platforms.

Authors:  Bo-Jeng Wang; Pei-Yi Wu; Yun-Wen Chen; Yu-Tzu Chang; Noopur Bhore; Po-Fan Wu; Yung-Feng Liao
Journal:  J Vis Exp       Date:  2018-01-25       Impact factor: 1.355

Review 2.  ACS chemical neuroscience molecule spotlight on BMS-708163.

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2012-03-21       Impact factor: 4.418

Review 3.  Computational modeling and biomarker studies of pharmacological treatment of Alzheimer's disease (Review).

Authors:  Mubashir Hassan; Qamar Abbas; Sung-Yum Seo; Saba Shahzadi; Hany Al Ashwal; Nazar Zaki; Zeeshan Iqbal; Ahmed A Moustafa
Journal:  Mol Med Rep       Date:  2018-05-22       Impact factor: 2.952

4.  Visible-light mediated carbonyl trifluoromethylative amination as a practical method for the synthesis of β-trifluoromethyl tertiary alkylamines.

Authors:  Kavoos Kolahdouzan; Roopender Kumar; Matthew J Gaunt
Journal:  Chem Sci       Date:  2020-10-09       Impact factor: 9.825

5.  Conformational Models of APP Processing by Gamma Secretase Based on Analysis of Pathogenic Mutations.

Authors:  Meewhi Kim; Ilya Bezprozvanny
Journal:  Int J Mol Sci       Date:  2021-12-18       Impact factor: 5.923
  5 in total

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