The development of tubulin-targeting biomolecules as anticancer agents has
been widely studied, and a variety of drugs are being clinically used and others are
being tested, including paclitaxel, docetaxel, laulimalide, peloruside, ixabepilone,
patupilone, vinblastine, vincristine, vinorelbine, vinflunine, colchicine, combretastatin,
and 2-methoxy estradiol. These agents target four distinct binding sites: laulimalide,
taxane/epothilone, vinca alkaloid, and colchicine. The dynamics of microtubule
polymerization have been identified as fascinating and well-established targets in
cancer therapy, since microtubule polymerization greatly impacts crucial processes,
such as mitosis. This chapter provides a comprehensive overview of biomolecules
targeting tubulin, detailing their chemistry, molecular mechanisms, and therapeutic
potential. It explores recent advances in the field and offers insights into the future
prospects of these biomolecules. This chapter describes the structure and function of
tubulin involved in cell division, and how blocking its function can effectively inhibit
cancer cell growth. Moreover, it discusses how tubulin-targeting agents have advanced
from natural products to synthetic and semi-synthetic derivatives in recent years, and
examines how drug design and delivery systems have improved specificity and
minimized toxicity, thus highlighting their potential as oncology therapies.
Keywords: Anticancer, Colchicine, Epothilone, Laulimalide, Microtubule, Microtubule-targeting agents, Taxol, Vinca alkaloid.
