Literature DB >> 19950987

Identification of cell-active lysine specific demethylase 1-selective inhibitors.

Rie Ueda1, Takayoshi Suzuki, Koshiki Mino, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata.   

Abstract

Lysine specific demethylase 1 (LSD1) plays a key role in the regulation of gene expression by removing the methyl groups from methylated Lys4 of histone H3 (H3K4). Here we report the identification of the first small-molecule LSD1-selective inhibitors. These inhibitors show in vivo H3K4-methylating activity and antiproliferative activity and should be useful as lead structures for anticancer drugs and as tools for studying the biological roles of LSD1.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19950987     DOI： 10.1021/ja907055q

Source DB:  PubMed          Journal:  J Am Chem Soc        ISSN： 0002-7863            Impact factor:   15.419


  62 in total

1.  Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia.

Authors:  Tino Schenk; Weihsu Claire Chen; Stefanie Göllner; Louise Howell; Liqing Jin; Katja Hebestreit; Hans-Ulrich Klein; Andreea C Popescu; Alan Burnett; Ken Mills; Robert A Casero; Laurence Marton; Patrick Woster; Mark D Minden; Martin Dugas; Jean C Y Wang; John E Dick; Carsten Müller-Tidow; Kevin Petrie; Arthur Zelent
Journal:  Nat Med       Date:  2012-03-11       Impact factor: 53.440

Review 2.  Structural insights into histone lysine demethylation.

Authors:  Haifeng Hou; Hongtao Yu
Journal:  Curr Opin Struct Biol       Date:  2010-10-21       Impact factor: 6.809

Review 3.  Chemical and biochemical approaches in the study of histone methylation and demethylation.

Authors:  Keqin Kathy Li; Cheng Luo; Dongxia Wang; Hualiang Jiang; Y George Zheng
Journal:  Med Res Rev       Date:  2012-07       Impact factor: 12.944

Review 4.  The redox basis of epigenetic modifications: from mechanisms to functional consequences.

Authors:  Anthony R Cyr; Frederick E Domann
Journal:  Antioxid Redox Signal       Date:  2011-02-05       Impact factor: 8.401

Review 5.  Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases.

Authors:  Zhanxin Wang; Dinshaw J Patel
Journal:  Q Rev Biophys       Date:  2013-09-02       Impact factor: 5.318

6.  Histone demethylases and their roles in cancer epigenetics.

Authors:  Alexandra D'Oto; Qing-Wu Tian; Andrew M Davidoff; Jun Yang
Journal:  J Med Oncol Ther       Date:  2016

Review 7.  The promise and failures of epigenetic therapies for cancer treatment.

Authors:  Pasano Bojang; Kenneth S Ramos
Journal:  Cancer Treat Rev       Date:  2013-07-05       Impact factor: 12.111

8.  Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity.

Authors:  Martin L Schmitt; Alexander-Thomas Hauser; Luca Carlino; Martin Pippel; Johannes Schulz-Fincke; Eric Metzger; Dominica Willmann; Teresa Yiu; Michelle Barton; Roland Schüle; Wolfgang Sippl; Manfred Jung
Journal:  J Med Chem       Date:  2013-09-05       Impact factor: 7.446

Review 9.  KDM1 class flavin-dependent protein lysine demethylases.

Authors:  Jonathan M Burg; Jennifer E Link; Brittany S Morgan; Frederick J Heller; Amanda E Hargrove; Dewey G McCafferty
Journal:  Biopolymers       Date:  2015-07       Impact factor: 2.505

10.  The lysine specific demethylase-1 (LSD1/KDM1A) regulates VEGF-A expression in prostate cancer.

Authors:  Vasundhra Kashyap; Shafqat Ahmad; Emeli M Nilsson; Leszek Helczynski; Sinéad Kenna; Jenny Liao Persson; Lorraine J Gudas; Nigel P Mongan
Journal:  Mol Oncol       Date:  2013-01-19       Impact factor: 6.603
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.