BTB-1: A Small Molecule Inhibitor of the Mitotic Motor Protein Kif18A

被引：52
|
作者：
Catarinella, Mario [1 ]
Gruener, Tamara [2 ]
Strittmatter, Tobias [1 ]
Marx, Andreas [1 ]
Mayer, Thomas U. [1 ]
机构：
[1] Univ Konstanz, Konstanz Res Sch Chem Biol, D-78457 Constance, Germany
[2] London Res Inst, Lincolns Inn Fields Labs, London WC2A 3PX, England
来源：
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2009年 / 48卷 / 48期
关键词：
antiproliferation; enzymes; inhibitors; mitosis; molecular motors; KINESIN EG5; CHROMOSOME ALIGNMENT; CELL-DIVISION; SPINDLE; POLO-LIKE-KINASE-1; MICROTUBULES;
D O I：
10.1002/anie.200904510
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Turning the motor off: A malachite green based assay leads to the identification of BTB-1 (see picture), the first small-molecule inhibitor of the mitotic motor protein Kif18A. BTB-1 reversibly inhibits the ATPase activity of the recombinant motor domain of Kif18A in vitro (see picture; red microtubules, blue/black structure = Kif18A) and will be a valuable tool to dissect the mechanochemical properties of Kif18A. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码：9072 / 9076
页数：5
相关论文
共 50 条
  • [1] Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers
    Marc Payton
    Brian Belmontes
    Kelly Hanestad
    Jodi Moriguchi
    Kui Chen
    John D. McCarter
    Grace Chung
    Maria Stefania Ninniri
    Jan Sun
    Raffi Manoukian
    Stuart Chambers
    Seok-Man Ho
    Robert J. M. Kurzeja
    Katheryne Z. Edson
    Upendra P. Dahal
    Tian Wu
    Sharon Wannberg
    Pedro J. Beltran
    Jude Canon
    Andrew S. Boghossian
    Matthew G. Rees
    Melissa M. Ronan
    Jennifer A. Roth
    Sheroy Minocherhomji
    Matthew P. Bourbeau
    Jennifer R. Allen
    Angela Coxon
    Nuria A. Tamayo
    Paul E. Hughes
    Nature Cancer, 2024, 5 : 66 - 84
  • [2] Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers
    Payton, Marc
    Belmontes, Brian
    Hanestad, Kelly
    Moriguchi, Jodi
    Chen, Kui
    Mccarter, John D.
    Chung, Grace
    Ninniri, Maria Stefania
    Sun, Jan
    Manoukian, Raffi
    Chambers, Stuart
    Ho, Seok-Man
    Kurzeja, Robert J. M.
    Edson, Katheryne Z.
    Dahal, Upendra P.
    Wu, Tian
    Wannberg, Sharon
    Beltran, Pedro J.
    Canon, Jude
    Boghossian, Andrew S.
    Rees, Matthew G.
    Ronan, Melissa M.
    Roth, Jennifer A.
    Minocherhomji, Sheroy
    Bourbeau, Matthew P.
    Allen, Jennifer R.
    Coxon, Angela
    Tamayo, Nuria A.
    Hughes, Paul E.
    NATURE CANCER, 2024, 5 (01) : 66 - 84
  • [3] Therapeutic targeting of the KIF18A motor protein in cancers with chromosomal instability
    Nature Cancer, 2024, 5 : 10 - 11
  • [4] Therapeutic targeting of the KIF18A motor protein in cancers with chromosomal instability
    Payton, Marc
    Hughes, Paul E.
    NATURE CANCER, 2024, 5 (01) : 10 - 11
  • [5] Sumoylation of Kif18A plays a role in regulating mitotic progression
    Feikun Yang
    Yan Chen
    Wei Dai
    BMC Cancer, 15
  • [6] Targeting the mitotic kinesin, KIF18A, in chromosomally unstable cancers
    Joseph, James D.
    Schutt, Katherine
    Fisher, Kira
    Queen, Katelyn
    Budington, Olivia
    Mao, Weifeng
    Liu, Wei
    Zhu, Zhengqing
    Zhang, Xiangping
    Xiao, Yisong
    Lai, Kunmin
    Gu, Xiaohui
    Stumpff, Jason
    Aswad, Fred
    CANCER RESEARCH, 2023, 83 (07)
  • [7] Sumoylation of Kif18A plays a role in regulating mitotic progression
    Yang, Feikun
    Chen, Yan
    Dai, Wei
    BMC CANCER, 2015, 15
  • [8] Kinesin-binding protein (KBP) is an inhibitory regulator of the mitotic kinesins Kif18A and Kif15.
    Malaby, H. L.
    Dumas, M.
    Stumpff, J.
    Ohi, R.
    MOLECULAR BIOLOGY OF THE CELL, 2017, 28
  • [9] Phosphorylation of KIF18A Alters Its Mitotic Function and Localization
    Queen, Katelyn A.
    Vandal, Sarah
    Thompson, Alex F.
    Stumpff, Jason K.
    BIOPHYSICAL JOURNAL, 2021, 120 (03) : 166A - 166A
  • [10] The kinesin-8 motor Kif18A suppresses kinetochore movements to control mitotic chromosome alignment
    Stumpff, Jason
    von Dassow, George
    Wagenbach, Michael
    Asbury, Charles
    Wordeman, Linda
    DEVELOPMENTAL CELL, 2008, 14 (02) : 252 - 262
12345