A protocol for high-throughput screening of histone lysine demethylase 4 inhibitors using TR-FRET assay

被引：2

作者：

Wu, Qiong ^{[1
]}

Lin, Wenwei ^{[2
]}

Li, Zhen-Mei ^{[3
]}

Rankovic, Zoran ^{[2
]}

White, Stephen W. ^{[3
,4
]}

Chen, Taosheng ^{[2
]}

Yang, Jun ^{[1
]}

机构：

[1] St Jude Childrens Res Hosp, Dept Surg, 262 Danny Thomas Pl, Memphis, TN 38105 USA

[2] St Jude Childrens Res Hosp, Dept Chem Biol & Therapeut, 262 Danny Thomas Pl, Memphis, TN 38105 USA

[3] St Jude Childrens Res Hosp, Dept Struct Biol, 262 Danny Thomas Pl, Memphis, TN 38105 USA

[4] St Jude Childrens Res Hosp, Grad Sch Biomed Sci, 262 Danny Thomas Pl, Memphis, TN 38105 USA

来源：

STAR PROTOCOLS | 2021年 / 2卷 / 03期

关键词：

Cancer; Chemistry; High Throughput Screening; Molecular/Chemical Probes; Protein Biochemistry; Protein expression and purification; Structural Biology;

D O I：

10.1016/j.xpro.2021.100702

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Identification of diverse chemotypes of selective KDM4 inhibitors is important for exploring and validating the roles of KDM4s in the pathogenesis of human disease and for developing therapies. Here, we report a protocol for high -throughput screening of KDM4 inhibitors using TR-FRET demethylation func-tional assay. We describe this protocol for screen of KDM4B inhibitors, which can be modified to screen inhibitors of other JmjC-domain-containing KDMs. For complete details on the use and execution of this protocol, please refer to Singh et al. (2021).

引用

页数：10

共 50 条

[31] HIGH-THROUGHPUT SCREENING ASSAY FOR INHIBITORS OF RAS FARNESYL TRANSFERASE
BERESINI, MH
YEH, SH
CHANG, AC
YEN, R
GALLOWAY, AL
WONG, WL
MARSTERS, JC
FASEB JOURNAL, 1995, 9 (06): : A1315 - A1315
[32] A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening
Wigle, Tim J.
Swinger, Kerren K.
Campbell, John E.
Scholle, Michael D.
Sherrill, John
Admirand, Elizabeth A.
Boriack-Sjodin, P. Ann
Kuntz, Kevin W.
Chesworth, Richard
Moyer, Mikel P.
Scott, Margaret Porter
Copeland, Robert A.
JOURNAL OF BIOMOLECULAR SCREENING, 2015, 20 (06) : 810 - 820
[33] Identification of Inhibitors of a Bacterial Sigma Factor Using a New High-Throughput Screening Assay
El-Mowafi, S. A.
Sineva, E.
Alumasa, J. N.
Nicoloff, H.
Tomsho, J. W.
Ades, S. E.
Keiler, K. C.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2015, 59 (01) : 193 - 205
[34] High-Throughput Screening for Inhibitors of the SARS-CoV-2 Protease Using a FRET-Biosensor
Brown, Alistair S.
Ackerley, David F.
Calcott, Mark J.
MOLECULES, 2020, 25 (20):
[35] A fluorogenic histone deacetylase assay well suited for high-throughput activity screening
Wegener, D
Wirsching, F
Riester, D
Schwienhorst, A
CHEMISTRY & BIOLOGY, 2003, 10 (01): : 61 - 68
[36] Development of FRET-based high-throughput screening for viral RNase III inhibitors
Wang, Linping
Saarela, Jani
Poque, Sylvain
Valkonen, Jari P. T.
MOLECULAR PLANT PATHOLOGY, 2020, 21 (07) : 961 - 974
[37] A robust bacterial assay for high-throughput screening of human 4-hydroxyphenylpyruvate dioxygenase inhibitors
Neuckermans, Jessie
Mertens, Alan
De Win, Dinja
Schwaneberg, Ulrich
De Kock, Joery
SCIENTIFIC REPORTS, 2019, 9 (1)
[38] A robust bacterial assay for high-throughput screening of human 4-hydroxyphenylpyruvate dioxygenase inhibitors
Jessie Neuckermans
Alan Mertens
Dinja De Win
Ulrich Schwaneberg
Joery De Kock
Scientific Reports, 9
[39] Protocol for high-throughput screening of SARS-CoV-2 main protease inhibitors using a robust fluorescence polarization assay
Zhang, Jing
Yan, Haohao
Yan, Gangan
Liu, Xiaoping
Wang, Yanchang
Chen, Yunyu
STAR PROTOCOLS, 2022, 3 (04):
[40] A high-throughput screening assay for dipeptidyl peptidase-IV inhibitors using human plasma
Zhang, Jing
Qian, Xing-Kai
Song, Pei-Fang
Li, Xiao-Dong
Wang, An-Qi
Huo, Hong
Yao, Jing-Chun
Zhang, Gui-Min
Zou, Li-Wei
ANALYTICAL METHODS, 2021, 13 (24) : 2671 - 2678

← 1 2 3 4 5 →