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Interaction of colchicine analogues with purified tubulin
Author(s) -
Choudhury Goutam Ghosh,
Banerjee Ashok,
Bhattacharyya Bhabatarak,
Biswas Birendra B.
Publication year - 1983
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(83)80729-7
Subject(s) - tropone , tubulin , colchicine , chemistry , titration , stereochemistry , fluorescence anisotropy , fluorescence , binding constant , microtubule , binding site , biophysics , biochemistry , biology , organic chemistry , genetics , physics , quantum mechanics , membrane , microbiology and biotechnology
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 K d 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 × 10 6 M −1 for desacetamidocolchicine, and 0.9 and 0.58 × 10 6 M −1 for 2‐methoxy‐5‐(2′,3′,4′‐trimethoxyphenyl) tropone.