Literature DB >> 26794039

Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide.

Taeko Kakizawa1, Tamio Mizukami2, Yukihiro Itoh3, Makoto Hasegawa2, Ryuzo Sasaki2, Takayoshi Suzuki4.   

Abstract

Lysine-specific demethylase 2 (LSD2) demethylates mono- and dimethylated Lys-4 of histone H3 (H3K4me1 and H3K4me2). NPAC protein is known to interact with LSD2 and promote its H3K4 demethylase activity. In this study, we established a demethylation assay system that utilizes recombinant LSD2 in the presence of a synthetic NPAC peptide. Several phenylcyclopropylamine (PCPA)-based inhibitors were examined for their LSD2 inhibitory activity in the LSD2 enzymatic assay with the NPAC peptide. The assay results showed that the PCPA derivatives, including NCD41, selectively inhibited LSD1 in preference to LSD2.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Histone H3K4 demethylation; Inhibitor; Lysine-specific demethylases 1 and 2 (LSD1 and LSD2); NPAC peptide

Mesh：

Substances：

Year:  2016        PMID： 26794039     DOI： 10.1016/j.bmcl.2016.01.036

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


  5 in total

1.  Activity-dependent Regulation of Histone Lysine Demethylase KDM1A by a Putative Thiol/Disulfide Switch.

Authors:  Emily L Ricq; Jacob M Hooker; Stephen J Haggarty
Journal:  J Biol Chem       Date:  2016-09-15       Impact factor: 5.157

Review 2.  Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases.

Authors:  Hideaki Niwa; Takashi Umehara
Journal:  Epigenetics       Date:  2017-02-10       Impact factor: 4.528

3.  Identification of ryuvidine as a KDM5A inhibitor.

Authors:  Eishin Mitsui; Shogo Yoshida; Yui Shinoda; Yasumasa Matsumori; Hiroshi Tsujii; Mie Tsuchida; Shuichi Wada; Makoto Hasegawa; Akihiro Ito; Koshiki Mino; Tetsuo Onuki; Minoru Yoshida; Ryuzo Sasaki; Tamio Mizukami
Journal:  Sci Rep       Date:  2019-07-09       Impact factor: 4.379

4.  Structure-Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2.

Authors:  Hideaki Niwa; Chiduru Watanabe; Shin Sato; Toshiyuki Harada; Hisami Watanabe; Ryo Tabusa; Shunsuke Fukasawa; Ayane Shiobara; Tomoko Hashimoto; Osamu Ohno; Kana Nakamura; Keiko Tsuganezawa; Akiko Tanaka; Mikako Shirouzu; Teruki Honma; Kenji Matsuno; Takashi Umehara
Journal:  ACS Med Chem Lett       Date:  2022-08-18       Impact factor: 4.632

Review 5.  Epigenetic assays for chemical biology and drug discovery.

Authors:  Sheraz Gul
Journal:  Clin Epigenetics       Date:  2017-04-21       Impact factor: 6.551
  5 in total

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