Interaction of colchicine analogues with purified tubulin

Goutam Ghosh Choudhury, Ashok Banerjee, Bhabatarak Bhattacharyya, Birendra B. Biswas

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

Binding of two colchicine analogues, desacetamidocolchicine and 2-methoxy-5-(2′,3′,4′-trimethoxyphenyl) tropone to purified tubulin have been studied. Both analogues bind to tubulin with a significant increase in fluorescence polarization of the drugs in solutions containing tubulin. The Kd for tubulin-drug complexes were found to be 1.25 × 10-6 M and 1.08 × 10-6 M for desacetamidocolchicine and 2-methoxy-5-(2′,3′,4′-trimethoxyphenyl) tropone, respectively. Scatchard analysis of the fluorescence titration curve of drug tubulin interaction also gives the values of stoichiometry and affinity constant. These were 0.8 and 1.6 × 106 M-1 for desacetamidocolchicine, and 0.9 and 0.58 × 106 M-1 for 2-methoxy-5-(2′,3′,4′-trimethoxyphenyl) tropone.

Original languageEnglish (US)
Pages (from-to)55-59
Number of pages5
JournalFEBS Letters
Volume161
Issue number1
DOIs
StatePublished - Sep 5 1983
Externally publishedYes

Keywords

  • B-ring of colchicine
  • Binding parameter
  • Brain tubulin
  • Fluorescence
  • Polarization

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

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