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  • Interaction of novel thiocolchicine analogs with the tubulin isoforms from bovine brain.

Interaction of novel thiocolchicine analogs with the tubulin isoforms from bovine brain.

Biochemical and biophysical research communications (1999-01-27)
A Banerjee, L T Kasmala, E Hamel, L Sun, K H Lee
ABSTRACT

The antimitotic alkaloid colchicine binds to tubulin and inhibits microtubule assembly. Recently a new series of colchicine derivatives has been synthesized in which the seven-membered B-ring was shortened to a six-membered ring. In an effort to study the role of the B-ring substituents in this new series, we have studied the interaction of two compounds of this series, THC 5 and THC 18, with tubulin isoforms from bovine brain. We find that THC 18, which has a side chain with a pi-bonded SP2 conformation, binds differently to the tubulin isoforms, while THC 5 with a slightly different side chain does not. The results indicate that the conformation of the B-ring domain plays a major role in the differential interaction of a colchicine derivative with different tubulin isoforms. The results will be very important in designing potent antitumor derivatives of colchicine.

MATERIALS
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Brand
Product Description

Sigma-Aldrich
Thiocolchicine, ≥97% (HPLC)