Mass Spectrometric Binding Study on Novel Anticancer Agents as Tubulin Depolymerizer

摘要

A new LC/MS/MS technique was developed for the determination of the degree of tubulin binding (concentration of unbound ligands) of anticancer agents used as tubulin depolymerizers. The method involves a simple step of separating unbound ligand from the marcomolecules (using ultrafiltration), followed by SRM using characteristics mass transitions. Of nine new, novel compounds studied four exhibited tubulin binding of > 55% (at 1.3 mg/mL tubulin concentration), four showed tubulin binding of 6-28%, and one did not bind at all. This new binding assay may be used as a screening tool for potential tubulin inhibitors.