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 language | English (US) |
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Pages (from-to) | 55-59 |
Number of pages | 5 |
Journal | FEBS Letters |
Volume | 161 |
Issue number | 1 |
DOIs | |
State | Published - Sep 5 1983 |
Externally published | Yes |
Keywords
- B-ring of colchicine
- Binding parameter
- Brain tubulin
- Fluorescence
- Polarization
ASJC Scopus subject areas
- Biophysics
- Structural Biology
- Biochemistry
- Molecular Biology
- Genetics
- Cell Biology