Literature DB >> 15267231

Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase.

Frédéric Bihel1, Chittaranjan Das, Michael J Bowman, Michael S Wolfe.   

Abstract

Gamma-secretase is the second of two proteolytic enzymes responsible for the release of the amyloid beta-peptide implicated in the etiology of Alzheimer's disease. Here, we used solid-phase synthesis to generate a new series of helical peptides as gamma-secretase inhibitors, one of which, 11, showed an IC(50) of 140 pM in a cell-free enzyme assay.

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Year:  2004        PMID: 15267231     DOI: 10.1021/jm049788c

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


  21 in total

Review 1.  Therapeutic approaches to modulating Notch signaling: current challenges and future prospects.

Authors:  Casper Groth; Mark E Fortini
Journal:  Semin Cell Dev Biol       Date:  2012-01-30       Impact factor: 7.727

2.  The initial substrate-binding site of gamma-secretase is located on presenilin near the active site.

Authors:  Anna Y Kornilova; Frédéric Bihel; Chittaranjan Das; Michael S Wolfe
Journal:  Proc Natl Acad Sci U S A       Date:  2005-02-18       Impact factor: 11.205

Review 3.  Unraveling the complexity of γ-secretase.

Authors:  Michael S Wolfe
Journal:  Semin Cell Dev Biol       Date:  2020-01-21       Impact factor: 7.727

4.  Inhibitors of signal peptide peptidase (SPP) affect HSV-1 infectivity in vitro and in vivo.

Authors:  Sariah J Allen; Kevin R Mott; Homayon Ghiasi
Journal:  Exp Eye Res       Date:  2014-04-24       Impact factor: 3.467

Review 5.  Toward the structure of presenilin/γ-secretase and presenilin homologs.

Authors:  Michael S Wolfe
Journal:  Biochim Biophys Acta       Date:  2013-12

6.  Distinct pharmacological effects of inhibitors of signal peptide peptidase and gamma-secretase.

Authors:  Toru Sato; Kuppanna Ananda; Cathy I Cheng; Eric J Suh; Saravanakumar Narayanan; Michael S Wolfe
Journal:  J Biol Chem       Date:  2008-10-01       Impact factor: 5.157

Review 7.  Taking the plunge: integrating structural, enzymatic and computational insights into a unified model for membrane-immersed rhomboid proteolysis.

Authors:  Sinisa Urban
Journal:  Biochem J       Date:  2010-01-15       Impact factor: 3.857

Review 8.  Toward structural elucidation of the gamma-secretase complex.

Authors:  Huilin Li; Michael S Wolfe; Dennis J Selkoe
Journal:  Structure       Date:  2009-03-11       Impact factor: 5.006

Review 9.  BACE and gamma-secretase characterization and their sorting as therapeutic targets to reduce amyloidogenesis.

Authors:  Neville Marks; Martin J Berg
Journal:  Neurochem Res       Date:  2009-09-17       Impact factor: 3.996

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

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