Literature DB >> 15050642

Parallel synthesis of DAPT derivatives and their gamma-secretase-inhibitory activity.

Toshiyuki Kan1, Yusuke Tominari, Kentaro Rikimaru, Yuichi Morohashi, Hideaki Natsugari, Taisuke Tomita, Takeshi Iwatsubo, Tohru Fukuyama.   

Abstract

Parallel synthesis of the C-terminal-modified DAPT (1) derivatives was accomplished utilizing our novel resin 7. Condensation reaction of the N-acylamino acid 10 with the amines 11a-o proceeded smoothly to give the corresponding amides 6a-o without any epimerization. Among the analogues, the benzophenonemethyl amide derivative 6o showed 30 times more potent activity than the original DAPT (1).

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Year:  2004        PMID: 15050642     DOI: 10.1016/j.bmcl.2004.01.067

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


  9 in total

1.  Participation of transmembrane domain 1 of presenilin 1 in the catalytic pore structure of the γ-secretase.

Authors:  Shizuka Takagi; Aya Tominaga; Chihiro Sato; Taisuke Tomita; Takeshi Iwatsubo
Journal:  J Neurosci       Date:  2010-11-24       Impact factor: 6.167

2.  Cooperative roles of hydrophilic loop 1 and the C-terminus of presenilin 1 in the substrate-gating mechanism of γ-secretase.

Authors:  Shizuka Takagi-Niidome; Tomoki Sasaki; Satoko Osawa; Takeshi Sato; Kanan Morishima; Tetsuo Cai; Takeshi Iwatsubo; Taisuke Tomita
Journal:  J Neurosci       Date:  2015-02-11       Impact factor: 6.167

3.  Expression and role of Notch signalling in the regeneration of rat tracheal epithelium.

Authors:  X-B Ma; X-S Jia; Y-L Liu; L-L Wang; S-L Sun; N Song; E-H Wang; F Li
Journal:  Cell Prolif       Date:  2009-02       Impact factor: 6.831

Review 4.  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

5.  N-{N-[2-(3,5-Difluorophenyl)acetyl]-(S)-alanyl}-(S)-phenylglycine tert-butyl ester (DAPT): an inhibitor of γ-secretase, revealing fine electronic and hydrogen-bonding features.

Authors:  Andrzej Czerwinski; Francisco Valenzuela; Pavel Afonine; Miroslawa Dauter; Zbigniew Dauter
Journal:  Acta Crystallogr C       Date:  2010-11-06       Impact factor: 1.172

6.  Presenilin-dependent intramembrane cleavage of ephrin-B1.

Authors:  Taisuke Tomita; Sayaka Tanaka; Yuichi Morohashi; Takeshi Iwatsubo
Journal:  Mol Neurodegener       Date:  2006-06-12       Impact factor: 14.195

7.  Binding of longer Aβ to transmembrane domain 1 of presenilin 1 impacts on Aβ42 generation.

Authors:  Yu Ohki; Naoaki Shimada; Aya Tominaga; Satoko Osawa; Takuya Higo; Satoshi Yokoshima; Tohru Fukuyama; Taisuke Tomita; Takeshi Iwatsubo
Journal:  Mol Neurodegener       Date:  2014-01-13       Impact factor: 14.195

8.  Genetic engineering approaches for the fermentative production of phenylglycines.

Authors:  David Moosmann; Vladislav Mokeev; Andreas Kulik; Natalie Osipenkov; Susann Kocadinc; Regina Ort-Winklbauer; Franziska Handel; Oliver Hennrich; Jung-Won Youn; Georg A Sprenger; Yvonne Mast
Journal:  Appl Microbiol Biotechnol       Date:  2020-02-20       Impact factor: 4.813

9.  Conformational Changes in Transmembrane Domain 4 of Presenilin 1 Are Associated with Altered Amyloid-β 42 Production.

Authors:  Aya Tominaga; Tetsuo Cai; Shizuka Takagi-Niidome; Takeshi Iwatsubo; Taisuke Tomita
Journal:  J Neurosci       Date:  2016-01-27       Impact factor: 6.167

  9 in total

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