The interaction of microtubules with stabilizers characterized at biochemical and structural levels

Abstract

Since the discovery of paclitaxel and its peculiar mechanism of cytotoxicity, which has made it and its analogues widely used antitumour drugs, a large effort has been done to understand the way they produce their effect in microtubules and to find other products that share this effect without their undesired side effects of (low solubility and development of multidrug resistance by tumour cells). This chapter reviews the actual knowledge about the biochemical and structural mechanisms of microtubule stabilization by microtubule stabilizing agents, and illustrates the way paclitaxel and its biomimetics induce microtubule assembly, the thermodynamics of their binding, the way they reach their binding site and the conformation they have when bound