Selective, covalent modification of β-tubulin residue Cys-239 by T138067, an antitumor agent with <i>in vivo</i> efficacy against multidrug-resistant tumors

Abstract excerpt

Microtubules are linear polymers of alpha- and beta-tubulin heterodimers and are the major constituents of mitotic spindles, which are essential for the separation of chromosomes during mitosis. Here we describe a synthetic compound, 2-fluoro-1-methoxy-4-pentafluorophenylsulfonamidobenzene (T138067), which covalently and selectively modifies the beta1, beta2, and beta4 isotypes of beta-tubulin at a conserved...

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