4.5 Article

DHTP is an allosteric inhibitor of the kinesin-13 family of microtubule depolymerases

期刊

FEBS LETTERS
卷 588, 期 14, 页码 2315-2320

出版社

ELSEVIER SCIENCE BV
DOI: 10.1016/j.febslet.2014.05.024

关键词

Kinesin; Chemical inhibitor; Microtubule; Cell division; Enzyme

资金

  1. Canadian Institutes of Health Research (CIHR) [MOP-89877, MOP-97928]
  2. Fonds de recherche du Quebec - Sante (FRQS)
  3. FRQS doctoral fellowship award
  4. Fonds Perseverance (IRIC, UdeM)
  5. Canadian Center of Excellence in Commercialization and Research (CECR)
  6. Canada Foundation for Innovation
  7. FRQS

向作者/读者索取更多资源

The Kinesin-13 family of microtubule depolymerases is a major regulator of microtubule dynamics. RNA interference-induced knockdown studies have highlighted their importance in many cell division processes including spindle assembly and chromosome segregation. Since microtubule turnovers and most mitotic events are relatively rapid (in minutes or seconds), developing tools that offer faster control over protein functions is therefore essential to more effectively interrogate Kinesin-13 activities in living cells. Here, we report the identification and characterization of a selective allosteric Kinesin-13 inhibitor, DHTP. Using high resolution microscopy, we show that DHTP is cell permeable and can modulate microtubule dynamics in cells. (C) 2014 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.

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