Unusual tubulin-clustering ability of specifically c7-modified colchicine analogues

Chembiochem. 2013 Aug 19;14(12):1444-9. doi: 10.1002/cbic.201300143. Epub 2013 Jul 10.

Abstract

Highly cytotoxic C7-modified colchicine analogues, exemplified by tubuloclustin, promote microtubule disassembly followed by the formation of very stable tubulin clusters, both in vitro and in cells. The proposed mechanism of action of tubuloclustin and its analogues, beyond that of colchicine, includes additional specific interactions with the α-tubulin subunit.

Keywords: anticancer agents; apoptosis; colchicine; cytotoxicity; microtubules; tubulin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adamantane / analogs & derivatives*
  • Adamantane / chemistry
  • Adamantane / pharmacology
  • Animals
  • Cells, Cultured
  • Colchicine / analogs & derivatives*
  • Colchicine / chemistry
  • Colchicine / pharmacology*
  • Cytotoxins / chemistry
  • Cytotoxins / pharmacology
  • Flow Cytometry
  • Fluorescent Antibody Technique
  • HeLa Cells
  • Humans
  • Mice
  • Microscopy, Electron, Transmission
  • Molecular Structure
  • Protein Binding / drug effects
  • Tubulin / metabolism*

Substances

  • Cytotoxins
  • N-(7-adamant-2-yloxy-7-oxoheptanoyl)-N-deacetylcolchicine
  • Tubulin
  • Adamantane
  • Colchicine