Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors

被引：160

作者：

Ueda, Rie ^{[1
]}

Suzuki, Takayoshi ^{[1
]}

Mino, Koshiki ^{[2
]}

Tsumoto, Hiroki ^{[1
]}

Nakagawa, Hidehiko ^{[1
]}

Hasegawa, Makoto ^{[2
]}

Sasaki, Ryuzo ^{[3
]}

Mizukami, Tamio ^{[2
]}

Miyata, Naoki ^{[1
]}

机构：

[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Aichi 4678603, Japan

[2] Nagahama Inst Biosci Technol, Grad Sch Biosci, Shiga 5260829, Japan

[3] Frontier Pharma Inc, Shiga 5260829, Japan

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2009年 / 131卷 / 48期

基金：

日本学术振兴会;

关键词：

HISTONE DEMETHYLATION; LSD1; RESOLUTION;

D O I：

10.1021/ja907055q

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

(Chemical Equation Presented) 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. © 2009 American Chemical Society.

引用

页码：17536 / 17537

页数：2

共 50 条

[41] Development of 5-hydroxypyrazole derivatives as reversible inhibitors of lysine specific demethylase 1
Mould, Daniel P.
Bremberg, Ulf
Jordan, Allan M.
Geitmann, Matthis
Maiques-Diaz, Alba
McGonagle, Alison E.
Small, Helen F.
Somervaille, Tim C. P.
Ogilvie, Donald
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (14) : 3190 - 3195
[42] Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine
Suzuki, Takayoshi
Asaba, Tomomi
Imai, Erika
Tsumoto, Hiroki
Nakagawa, Hidehiko
Miyata, Naoki
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (19) : 5670 - 5672
[43] Discovery of a Novel Selective and Cell-Active N6-Methyladenosine RNA Demethylase ALKBH5 Inhibitor
Yang, Xianyuan
Huang, Kaitao
Wu, Xu-Nian
Zhang, Chen
Sun, Yixuan
Gao, Yanfeng
Zhou, Jiawang
Tao, Lijun
Zhang, Haisheng
Wu, Yinuo
Luo, Hai-Bin
Wang, Hongsheng
JOURNAL OF MEDICINAL CHEMISTRY, 2025, 68 (04) : 4133 - 4147
[44] A SELECTIVE LYSINE-SPECIFIC DEMETHYLASE 1 INHIBITOR SUPPRESSES TESTICULAR TUMOR PROLIFERATION
Etani, Toshiki
Naiki, Taku
Nozaki, Satoshi
Nagai, Takashi
Iida, Keitaro
Ando, Ryosuke
Kawai, Noriyasu
Takahashi, Satoru
Suzuki, Takayoshi
Yasui, Takahiro
JOURNAL OF UROLOGY, 2019, 201 (04): : E1064 - E1065
[45] Cell-Active, Reversible, and Irreversible Covalent Inhibitors That Selectively Target the Catalytic Lysine of BCR-ABL Kinase
Chen, Peng
Sun, Jie
Zhu, Chengjun
Tang, Guanghui
Wang, Wei
Xu, Manyi
Xiang, Menghua
Zhang, Chong-Jing
Zhang, Zhi-Min
Gao, Liqian
Yao, Shao Q.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2022, 61 (26)
[46] Development of Assays for Discovery of Cell-active Tankyrase Inhibitors
Chell, V.
Brooks, T.
Wayne, J.
Moore, J. D.
Brazier, H.
Shaw, T.
Baker, L.
Massey, A.
Graham, C.
Macias, A. T.
EUROPEAN JOURNAL OF CANCER, 2012, 48 : 124 - 124
[47] Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors
Siu, Tony
Liang, Jun
Arruda, Jeannie
Li, Yiwei
Jones, Raymond E.
Defeo-Jones, Deborah
Barnett, Stanley F.
Robinson, Ronald G.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2008, 18 (14) : 4186 - 4190
[48] Cell-active carbazole derivatives as inhibitors of the zika virus protease
Rassias, Gerasimos
Zogali, Vasiliki
Swarbrick, Crystall M. D.
Chan, Kitti Wing Ki
Chan, Shu Ann
Gwee, Chin Piaw
Wang, Sai
Kaplanai, Entzy
Canko, Aleksander
Kiousis, Dimitrios
Lescar, Julien
Luo, Dahai
Matsoukas, Minos-Timotheos
Vasudevan, Subhash G.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 180 : 536 - 545
[49] Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors
Shi, Ying
Wu, Yan-Ran
Su, Ming-Bo
Shen, Dong-Hao
Gunosewoyo, Hendra
Yang, Fan
Li, Jia
Tang, Jie
Zhou, Yu-Bo
Yu, Li-Fang
RSC ADVANCES, 2018, 8 (03): : 1666 - 1676
[50] Lysine-Specific Demethylase 1 (LSD1) Inhibitors: Peptides as an Emerging Class of Therapeutics
Baby, Stephin
Shinde, Suchita Dattatray
Kulkarni, Neeraj
Sahu, Bichismita
ACS CHEMICAL BIOLOGY, 2023, 18 (10) : 2144 - 2155

← 1 2 3 4 5 →