Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity

被引：9

作者：

Ourailidou, Maria E. ^{[1
]}

Lenoci, Alessia ^{[2
]}

Zwergel, Clemens ^{[2
]}

Rotili, Dante ^{[2
]}

Mai, Antonello ^{[2
,3
]}

Dekker, Frank J. ^{[1
]}

机构：

[1] Univ Groningen, Groningen Res Inst Pharm, Dept Chem & Pharmaceut Biol, Antonius Deusinglaan 1, NL-9713 AV Groningen, Netherlands

[2] Sapienza Univ, Dept Drug Chem & Technol, Ple A Moro 5, I-00185 Rome, Italy

[3] Sapienza Univ, Cenci Bolognetti Fdn, Pasteur Inst, Ple A Moro 5, I-00185 Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2017年 / 25卷 / 03期

基金：

欧洲研究理事会;

关键词：

Lysine demethylation; Tumorigenesis; Tranylcypromine; Irreversible inhibition; Enzyme labeling; LSD1 HISTONE DEMETHYLASE; THERAPEUTIC STRATEGY; BIOLOGICAL-ACTIVITY; STRUCTURAL BASIS; HDAC INHIBITORS; PROTEIN; DERIVATIVES; TRANYLCYPROMINE; TRANS-2-PHENYLCYCLOPROPYLAMINE; MECHANISMS;

D O I：

10.1016/j.bmc.2016.11.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The implications of lysine-specific demethylase-1 (LSD1) in tumorigenesis have urged scientists to develop diagnostic tools in order to explore the function of this enzyme. In this work, we present our efforts on the development of tranylcypromine (TCP)-based functionalized probes for activity -based protein profiling (ABPP) of LSD1 activity. Biotinylated forms of selected compounds enabled dose-dependent enzyme labeling of recombinant LSD1. However, treatment with LSD1 inhibitors did not clearly reduce the LSD1 labeling efficiency thus indicating that labeling using these probes is not activity dependent. This calls for alternative strategies to develop probes for ABPP of the enzyme LSD1. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：847 / 856

页数：10

共 50 条

[41] Novel Lysine-specific Demethylase 1 Inhibitor as a Potential Therapeutics for Glioblastoma
Shinjo, Keiko
Murofushi, Yoshiteru
Suzuki, Miho
Kondo, Yutaka
CANCER SCIENCE, 2024, 115 : 2077 - 2077
[42] Role of lysine-specific demethylase 1 in immunotherapy of gastric cancer: An update
Ren, Yongjing
Gong, Yanan
Zhao, Huan
You, Duo
Li, Zhifei
Wang, Sai-Qi
Chen, Xiaobing
CHINESE JOURNAL OF CANCER RESEARCH, 2024, 36 (06)
[43] Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin induction
Shi, Lihong
Cui, Shuaiying
Engel, James D.
Tanabe, Osamu
NATURE MEDICINE, 2013, 19 (03) : 291 - 294
[44] Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin induction
Lihong Shi
Shuaiying Cui
James D Engel
Osamu Tanabe
Nature Medicine, 2013, 19 : 291 - 294
[45] Expression of Lysine-specific demethylase 1 in human epithelial ovarian cancer
Chen, Cong
Ge, Jing
Lu, Qibin
Ping, Guoqiang
Yang, Chunqing
Fang, Xuefeng
JOURNAL OF OVARIAN RESEARCH, 2015, 8
[46] MicroRNA-137-mediated inhibition of lysine-specific demethylase-1 prevents against rheumatoid arthritis in an association with the REST/mTOR axis
Sun, Wei
Zhang, Yijun
Wang, Guanghui
MOLECULAR PAIN, 2021, 17
[47] Intermolecular insights into allosteric inhibition of histone lysine-specific demethylase 1
Zhang, Xiangyu
Sun, Yixiang
Zhang, Ziheng
Wang, Hanxun
Wang, Jian
Zhao, Dongmei
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS, 2021, 1865 (11):
[48] Lysine-Specific Demethylase 1 in Energy Metabolism: A Novel Target for Obesity
Wang, Dan
Kuang, Yanling
Zhang, Guolong
Xiao, Kan
Liu, Yulan
JOURNAL OF NUTRITION, 2022, 152 (07): : 1611 - 1620
[49] Lysine-Specific Demethylase 1 Regulates the Embryonic Transcriptome and CoREST Stability
Foster, Charles T.
Dovey, Oliver M.
Lezina, Larissa
Luo, Jin Li
Gant, Timothy W.
Barlev, Nick
Bradley, Allan
Cowley, Shaun M.
MOLECULAR AND CELLULAR BIOLOGY, 2010, 30 (20) : 4851 - 4863
[50] Expression of Lysine-specific demethylase 1 in human epithelial ovarian cancer
Cong Chen
Jing Ge
Qibin Lu
Guoqiang Ping
Chunqing Yang
Xuefeng Fang
Journal of Ovarian Research, 8

← 1 2 3 4 5 →