Interaction of colchicine analogues with purified tubulin

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

doi:10.1016/0014-5793(83)80729-7

Interaction of colchicine analogues with purified tubulin

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

Research output: Contribution to journal › Article

20 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 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 × 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)
Pages (from-to)	55-59
Number of pages	5
Journal	FEBS Letters
Volume	161
Issue number	1
DOIs	https://doi.org/10.1016/0014-5793(83)80729-7
State	Published - Sep 5 1983
Externally published	Yes

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Keywords

B-ring of colchicine
Binding parameter
Brain tubulin
Fluorescence
Polarization

ASJC Scopus subject areas

Biophysics
Structural Biology
Biochemistry
Molecular Biology
Genetics
Cell Biology

Cite this

Choudhury, G. G., Banerjee, A., Bhattacharyya, B., & Biswas, B. B. (1983). Interaction of colchicine analogues with purified tubulin. FEBS Letters, 161(1), 55-59. https://doi.org/10.1016/0014-5793(83)80729-7

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title = "Interaction of colchicine analogues with purified tubulin",

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.",

keywords = "B-ring of colchicine, Binding parameter, Brain tubulin, Fluorescence, Polarization",

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AU - Banerjee, Ashok

AU - Bhattacharyya, Bhabatarak

AU - Biswas, Birendra B.

PY - 1983/9/5

Y1 - 1983/9/5

N2 - 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.

AB - 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.

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10.1016/0014-5793(83)80729-7