Literature DB >> 15006396

KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.

Tooru Kimura1, Daisuke Shuto, Soko Kasai, Ping Liu, Koushi Hidaka, Takashi Hamada, Yoshio Hayashi, Chinatsu Hattori, Masashi Asai, Shinobu Kitazume, Takaomi C Saido, Shoichi Ishiura, Yoshiaki Kiso.   

Abstract

Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE1 inhibitor KMI-370 (IC(50)=3.4 nM) was designed and synthesized.

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Year:  2004        PMID: 15006396     DOI: 10.1016/j.bmcl.2003.12.088

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


  5 in total

1.  BACE1 Inhibitor Peptides: Can an Infinitely Small k cat Value Turn the Substrate of an Enzyme into Its Inhibitor?

Authors:  Yoshio Hamada; Shoichi Ishiura; Yoshiaki Kiso
Journal:  ACS Med Chem Lett       Date:  2011-12-26       Impact factor: 4.345

Review 2.  BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease.

Authors:  Arun K Ghosh; Heather L Osswald
Journal:  Chem Soc Rev       Date:  2014-10-07       Impact factor: 54.564

3.  Discovery of potent beta-secretase (bace-1) inhibitors by the synthesis of isophthalamide-containing hybrids.

Authors:  Yi-Ping Zhu; Kun Xiao; Hai-Ping Yu; Lan-Ping Ma; Bing Xiong; Hai-Yan Zhang; Xin Wang; Jing-Ya Li; Jia Li; Jing-Kang Shen
Journal:  Acta Pharmacol Sin       Date:  2009-01-26       Impact factor: 6.150

Review 4.  Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs.

Authors:  Riqiang Yan
Journal:  Transl Neurodegener       Date:  2016-07-14       Impact factor: 8.014

Review 5.  New directions for protease inhibitors directed drug discovery.

Authors:  Yoshio Hamada; Yoshiaki Kiso
Journal:  Biopolymers       Date:  2016-11-04       Impact factor: 2.505

  5 in total

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