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Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44.

Publication ,  Journal Article
Kahsai, AW; Zhu, S; Wardrop, DJ; Lane, WS; Fenteany, G
Published in: Chem Biol
September 2006

In the course of screening for new small-molecule modulators of cell motility, we discovered that quinocarmycin (also known as quinocarcin) analog DX-52-1 is an inhibitor of epithelial cell migration. While it has been assumed that the main target of DX-52-1 is DNA, we identified and confirmed radixin as the relevant molecular target of DX-52-1 in the cell. Radixin is a member of the ezrin/radixin/moesin family of membrane-actin cytoskeleton linker proteins that also participate in signal transduction pathways. DX-52-1 binds specifically and covalently to the C-terminal region of radixin, which contains the domain that interacts with actin filaments. Overexpression of radixin in cells abrogates their sensitivity to DX-52-1's antimigratory activity. Small interfering RNA-mediated silencing of radixin expression reduces the rate of cell migration. Finally, we found that DX-52-1 disrupts radixin's ability to interact with both actin and the cell adhesion molecule CD44.

Duke Scholars

Published In

Chem Biol

DOI

ISSN

1074-5521

Publication Date

September 2006

Volume

13

Issue

9

Start / End Page

973 / 983

Location

United States

Related Subject Headings

  • Transfection
  • RNA Interference
  • Protein Binding
  • Organic Chemistry
  • Mice
  • Membrane Proteins
  • Isoquinolines
  • Insecta
  • Inhibitory Concentration 50
  • Hyaluronan Receptors
 

Citation

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Kahsai, A. W., Zhu, S., Wardrop, D. J., Lane, W. S., & Fenteany, G. (2006). Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44. Chem Biol, 13(9), 973–983. https://doi.org/10.1016/j.chembiol.2006.07.011
Kahsai, Alem W., Shoutian Zhu, Duncan J. Wardrop, William S. Lane, and Gabriel Fenteany. “Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44.Chem Biol 13, no. 9 (September 2006): 973–83. https://doi.org/10.1016/j.chembiol.2006.07.011.
Kahsai AW, Zhu S, Wardrop DJ, Lane WS, Fenteany G. Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44. Chem Biol. 2006 Sep;13(9):973–83.
Kahsai, Alem W., et al. “Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44.Chem Biol, vol. 13, no. 9, Sept. 2006, pp. 973–83. Pubmed, doi:10.1016/j.chembiol.2006.07.011.
Kahsai AW, Zhu S, Wardrop DJ, Lane WS, Fenteany G. Quinocarmycin analog DX-52-1 inhibits cell migration and targets radixin, disrupting interactions of radixin with actin and CD44. Chem Biol. 2006 Sep;13(9):973–983.
Journal cover image

Published In

Chem Biol

DOI

ISSN

1074-5521

Publication Date

September 2006

Volume

13

Issue

9

Start / End Page

973 / 983

Location

United States

Related Subject Headings

  • Transfection
  • RNA Interference
  • Protein Binding
  • Organic Chemistry
  • Mice
  • Membrane Proteins
  • Isoquinolines
  • Insecta
  • Inhibitory Concentration 50
  • Hyaluronan Receptors