A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors

被引：3
|
作者：
Tsuji, Kohei [1 ,2 ]
Hymel, David [1 ]
Burke, Terrence R., Jr. [1 ]
机构：
[1] NIH, NCI, Chem Biol Lab, Ctr Canc Res, Frederick, MD 21702 USA
[2] Tokyo Med & Dent Univ TMDU, Dept Med Chem, Inst Biamatenals & Bioengn, Chiyoda Ku, 2-3-10 Kandasurugadai, Tokyo 1010062, Japan
来源：
ANALYTICAL METHODS | 2020年 / 12卷 / 36期
关键词：
BINDING ASSAY; BOX DOMAIN; POTENT; POLO-LIKE-KINASE-1; PLK1;
D O I：
10.1039/d0ay01223h
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
Using a probe consisting of a fluorescein-labeled variant of the potent polo-like kinase 1 (Plk1) inhibitor BI2536 [FITC-PEG-Lys(BI2536) 4], we were able to determine halfmaximal inhibitory concentration (IC50) of ATP-competitive Type 1 inhibitors of Plk1 by means of a fluorescence recovery assay. This methodology represents a cost-effective and simple alternative to traditional kinase assays for initial screening of potential Plk1 inhibitors.
引用
收藏
页码：4418 / 4421
页数：4
相关论文
共 50 条
  • [21] Development of a High Throughput Assay for Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1 Based on Time-Resolved Fluorescence Energy Transfer
    Kim, Tae Gi
    Lee, Ju Hee
    Lee, Mi Young
    Kima, Ka-Ul
    Lee, Jeong Hyun
    Park, Chi Hoon
    Lee, Byung Ho
    Oh, Kwang-Seok
    BIOLOGICAL & PHARMACEUTICAL BULLETIN, 2017, 40 (09) : 1454 - 1462
  • [22] Small-molecule inhibitors for targeting polo-like kinase 1
    Kolosenko, Iryna
    Palm-Apergi, Caroline
    FUTURE MEDICINAL CHEMISTRY, 2020, 12 (16) : 1457 - 1460
  • [23] Identification of Polo-like kinase 1 interaction inhibitors using a novel cell-based assay
    Normandin, Karine
    Lavallee, Jean-Francois
    Futter, Marie
    Beautrait, Alexandre
    Duchaine, Jean
    Guiral, Sebastien
    Marinier, Anne
    Archambault, Vincent
    SCIENTIFIC REPORTS, 2016, 6
  • [24] Identification of Polo-like kinase 1 interaction inhibitors using a novel cell-based assay
    Karine Normandin
    Jean-François Lavallée
    Marie Futter
    Alexandre Beautrait
    Jean Duchaine
    Sébastien Guiral
    Anne Marinier
    Vincent Archambault
    Scientific Reports, 6
  • [25] Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1
    Hornberger, Keith R.
    Badiang, Jennifer G.
    Salovich, James M.
    Kuntz, Kevin W.
    Emmitte, Kyle A.
    Cheung, Mui
    TETRAHEDRON LETTERS, 2008, 49 (44) : 6348 - 6351
  • [26] Structural analysis of PIM1 kinase complexes with ATP-competitive inhibitors
    Jozefina Bogusz
    Karol Zrubek
    Krzysztof P. Rembacz
    Przemyslaw Grudnik
    Przemyslaw Golik
    Malgorzata Romanowska
    Benedykt Wladyka
    Grzegorz Dubin
    Scientific Reports, 7
  • [27] QSAR models for predicting the bioactivity of Polo-like Kinase 1 inhibitors
    Kong, Yue
    Yan, Aixia
    CHEMOMETRICS AND INTELLIGENT LABORATORY SYSTEMS, 2017, 167 : 214 - 225
  • [28] SYNTHESIS OF SMALL PEPTIDE INHIBITORS TO THE POLO-BOX DOMAIN OF POLO-LIKE KINASE 1
    Ahn, M.
    Park, J. -E.
    Lee, K. S.
    Shin, S. Y.
    Bang, J. K.
    JOURNAL OF PEPTIDE SCIENCE, 2014, 20 : S155 - S155
  • [29] Structural analysis of PIM1 kinase complexes with ATP-competitive inhibitors
    Bogusz, Jozefina
    Zrubek, Karol
    Rembacz, Krzysztof P.
    Grudnik, Przemyslaw
    Golik, Przemyslaw
    Romanowska, Malgorzata
    Wladyka, Benedykt
    Dubin, Grzegorz
    SCIENTIFIC REPORTS, 2017, 7
  • [30] Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton
    Mita, Yusuke
    Noguchi-Yachide, Tomomi
    Ishikawa, Minoru
    Hashimoto, Yuichi
    BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (03) : 608 - 617
12345