Small-Molecule Inhibitors of Tubulin Polymerization: Recent Advances

Dear colleagues,

Although there have been exceptional advancements in targeted drugs and immunotherapies as highly effective cancer treatment modalities, molecules that interact with the tubulin-microtubule protein system remain one of the major treatment options in the clinic. This is due, in part, to their effectiveness against many tumor types and their high potency against diverse cancer cells. A significant number of approved tubulin inhibitors are known to date, functioning either as microtubule stabilizers or destabilizers. However, one of the major clinical limitations associated with many of these potent tubulin inhibitors relates to undesirable off-target toxicities. In response, there have been promising strategies developed to enhance selective tumor targeting including novel drug formulations, antibody–drug conjugates, prodrugs selective for tumors or components of the tumor microenvironment, along with other innovative drug delivery approaches. In parallel, another strategy centers on the discovery and development of next generation tubulin inhibitors that demonstrate inherently reduced toxicities through numerous strategies including the  incorporation of additional mechanisms of action(s), interaction with different (and often unique) binding sites on the tubulin-microtubule protein system, and synthetic modification of promising lead tubulin inhibitors, to name a few. This Special Issue aims to capture recent advancements in this historically rich, vibrant, and rapidly developing field of research. Contributions related to all aspects of therapeutic development associated with the tubulin-microtubule protein system are welcome, including computer-aided drug design, discovery of new tubulin inhibitors, and novel drug delivery strategies. Please note, manuscripts that report on the biological evaluation of mixtures of compounds, clinical studies or purely pharmacological studies that look deeper into the standard action of well-established drugs are less desirable for this Special Issue.

Prof. Dr. Kevin G. Pinney
Prof. Dr. Wei Li
Guest Editors

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• tubulin inhibitors
• drug resistance
• chemotherapy
• targeted therapies
• microtubules
• tubulin
• polymerization dynamics