Literature DB >> 22778845

ACS chemical neuroscience molecule spotlight on semagacestat (LY450139).

Corey R Hopkins1.   

Abstract

Semagacestat (LY450139) is a novel γ-secretase inhibitor currently in late-stage development by Eli Lilly and Company as a potential treatment for Alzheimer's disease (AD). Semagacestat is currently being studied in two phase III clinical trials.

Entities:  

Keywords:  AD; Alzheimer’s disease; Gamma-secretase; LY450139; neurodegeneration; semagacestat

Mesh：

Substances：

Year:  2010        PMID： 22778845      PMCID： PMC3368681          DOI： 10.1021/cn1000606

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


  9 in total

1.  Safety, tolerability, and changes in amyloid beta concentrations after administration of a gamma-secretase inhibitor in volunteers.

Authors:  Eric Siemers; Michael Skinner; Robert A Dean; Celedon Gonzales; Julie Satterwhite; Martin Farlow; Daniel Ness; Patrick C May
Journal:  Clin Neuropharmacol       Date:  2005 May-Jun       Impact factor: 1.592

2.  Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease.

Authors:  E R Siemers; J F Quinn; J Kaye; M R Farlow; A Porsteinsson; P Tariot; P Zoulnouni; J E Galvin; D M Holtzman; D S Knopman; J Satterwhite; C Gonzales; R A Dean; P C May
Journal:  Neurology       Date:  2006-02-28       Impact factor: 9.910

3.  Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase.

Authors:  Eric R Siemers; Robert A Dean; Stuart Friedrich; Lisa Ferguson-Sells; Celedon Gonzales; Martin R Farlow; Patrick C May
Journal:  Clin Neuropharmacol       Date:  2007 Nov-Dec       Impact factor: 1.592

4.  Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease.

Authors:  Adam S Fleisher; Rema Raman; Eric R Siemers; Lida Becerra; Christopher M Clark; Robert A Dean; Martin R Farlow; James E Galvin; Elaine R Peskind; Joseph F Quinn; Abdullah Sherzai; B Brooke Sowell; Paul S Aisen; Leon J Thal
Journal:  Arch Neurol       Date:  2008-08

5.  Presenilin 1 is required for Notch1 and DII1 expression in the paraxial mesoderm.

Authors:  P C Wong; H Zheng; H Chen; M W Becher; D J Sirinathsinghji; M E Trumbauer; H Y Chen; D L Price; L H Van der Ploeg; S S Sisodia
Journal:  Nature       Date:  1997-05-15       Impact factor: 49.962

6.  Natural oligomers of the amyloid-beta protein specifically disrupt cognitive function.

Authors:  James P Cleary; Dominic M Walsh; Jacki J Hofmeister; Ganesh M Shankar; Michael A Kuskowski; Dennis J Selkoe; Karen H Ashe
Journal:  Nat Neurosci       Date:  2004-12-19       Impact factor: 24.884

7.  Differential effects of gamma-secretase and BACE1 inhibition on brain Abeta levels in vitro and in vivo.

Authors:  Anders Brandt Elvang; Christiane Volbracht; Lars Østergaard Pedersen; Klaus Gjervig Jensen; Jens-Jakob Karlsson; Stine Anna Larsen; Arne Mørk; Tine Bryan Stensbøl; Jesper Frank Bastlund
Journal:  J Neurochem       Date:  2009-06-10       Impact factor: 5.372

Review 8.  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

Review 9.  Alzheimer's disease: from pathology to therapeutic approaches.

Authors:  Roland Jakob-Roetne; Helmut Jacobsen
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336
  9 in total
  6 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.  Initial Optimization of a New Series of γ-Secretase Modulators Derived from a Triterpene Glycoside.

Authors:  Nathan O Fuller; Jed L Hubbs; Wesley F Austin; Steffen P Creaser; Timothy D McKee; Robyn M B Loureiro; Barbara Tate; Weiming Xia; Jeffrey L Ives; Mark A Findeis; Brian S Bronk
Journal:  ACS Med Chem Lett       Date:  2012-08-29       Impact factor: 4.345

3.  Neurotrophic Peptides: Potential Drugs for Treatment of Amyotrophic Lateral Sclerosis and Alzheimer's disease.

Authors:  Jessica Ciesler; Youssef Sari
Journal:  Open J Neurosci       Date:  2013-04-08

Review 4.  ACS chemical neuroscience molecule spotlight on BMS-708163.

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

5.  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

6.  TrkA-mediated endocytosis of p75-CTF prevents cholinergic neuron death upon γ-secretase inhibition.

Authors:  María Luisa Franco; Irmina García-Carpio; Raquel Comaposada-Baró; Juan J Escribano-Saiz; Lucía Chávez-Gutiérrez; Marçal Vilar
Journal:  Life Sci Alliance       Date:  2021-02-03
  6 in total

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