Literature DB >> 20650635

Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library.

Motonori Kurosumi1, Yoshino Nishio, Satoko Osawa, Hisayoshi Kobayashi, Takeshi Iwatsubo, Taisuke Tomita, Hiroyuki Miyachi.   

Abstract

Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived gamma-secretase inhibitors (GSIs). Structure-activity relationship studies indicated that (R)-configuration of alpha-substituted phenylpropanoic acid structure and cinnamic acid structure is favorable to prepare Notch-sparing GSIs. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20650635     DOI: 10.1016/j.bmcl.2010.06.131

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


  2 in total

Review 1.  γ-Secretase inhibitors and modulators.

Authors:  Todd E Golde; Edward H Koo; Kevin M Felsenstein; Barbara A Osborne; Lucio Miele
Journal:  Biochim Biophys Acta       Date:  2013-06-17

2.  Inhibition of ADAM-17 more effectively down-regulates the Notch pathway than that of γ-secretase in renal carcinoma.

Authors:  Zhen Guo; Xunbo Jin; Haiyan Jia
Journal:  J Exp Clin Cancer Res       Date:  2013-05-09
  2 in total

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