Literature DB >> 18556202

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

Anthony Kreft1, 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.   

Abstract

Using a cell-based assay, we have identified a new series of Notch-sparing gamma-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved gamma-secretase inhibitory potency and Notch-sparing selectivity.

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Year:  2008        PMID： 18556202     DOI： 10.1016/j.bmcl.2008.05.064

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


  4 in total

1.  Molecular pathways: context-dependent approaches to Notch targeting as cancer therapy.

Authors:  Ann Marie Egloff; Jennifer R Grandis
Journal:  Clin Cancer Res       Date:  2012-07-06       Impact factor: 12.531

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

Authors:  Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2012-01-18       Impact factor: 4.418

3.  Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Authors:  Guriqbal S Basi; Susanna Hemphill; Elizabeth F Brigham; Anna Liao; Danielle L Aubele; Jeanne Baker; Robin Barbour; Michael Bova; Xiao-Hua Chen; Michael S Dappen; Tovah Eichenbaum; Erich Goldbach; Jon Hawkinson; Rose Lawler-Herbold; Kang Hu; Terence Hui; Jacek J Jagodzinski; Pamela S Keim; Dora Kholodenko; Lee H Latimer; Mike Lee; Jennifer Marugg; Matthew N Mattson; Scott McCauley; James L Miller; Ruth Motter; Linda Mutter; Martin L Neitzel; Huifang Ni; Lan Nguyen; Kevin Quinn; Lany Ruslim; Christopher M Semko; Paul Shapiro; Jenifer Smith; Ferdie Soriano; Balazs Szoke; Kevin Tanaka; Pearl Tang; John A Tucker; Xiacong Michael Ye; Mei Yu; Jing Wu; Ying-Zi Xu; Albert W Garofalo; John Michael Sauer; Andrei W Konradi; Daniel Ness; George Shopp; Michael A Pleiss; Stephen B Freedman; Dale Schenk
Journal:  Alzheimers Res Ther       Date:  2010-12-29       Impact factor: 6.982

4.  In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects.

Authors:  Lynn A Hyde; Qi Zhang; Robert A Del Vecchio; Prescott T Leach; Mary E Cohen-Williams; Lei Chen; Gwendolyn T Wong; Nansie A McHugh; Joseph Chen; Guy A Higgins; Theodros Asberom; Wei Li; Dmitri Pissarnitski; Diane Levitan; Amin A Nomeir; John W Clader; Lili Zhang; Eric M Parker
Journal:  Int J Alzheimers Dis       Date:  2013-03-14
  4 in total

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