Structures of a diverse set of colchicine binding site inhibitors in complex with tubulin provide a rationale for drug discovery

Microtubules are dynamic assemblies of αβ‐tubulin heterodimers and have been recognized as highly attractive targets for cancer chemotherapy. A broad range of agents bind to tubulin and interfere with microtubule assembly. Despite having a long history of characterization, colchicine binding site inhibitors ( CBSI s) have not yet reached the commercial phase as anti‐cancer drugs to date. We determined the structures of tubulin complexed with a...