Background: Microtubule Targeting Agents (MTAs) represent the most successful
anticancer drugs for cancer chemotherapy. Through interfering with the tubulin polymerization
and depolymerization dynamics, MTAs influence intracellular transport and cell signal pathways,
inhibit cell mitosis and cell proliferation, and induce cell apoptosis and death. The tubulin maytansine
site binding agents are natural or nature-derived products that represent one type of the
MTAs that inhibit tubulin polymerization and exhibit potent antitumor activity both in vitro and
in vivo. They are used as Antibody-Drug Conjugates (ADCs) in cancer chemotherapy.
Methods: Using SciFinder® as a tool, the publications about maytansine, its derivatives, maytansine
binding site, maytansine site binding agents and their applications as MTAs for cancer
therapy were surveyed with an exclusion on those published as patents. The latest progresses in
clinical trials were obtained from the clinical trial web.
Results: This article presents an introduction about MTAs, maytansine, maytansine binding site
and its ligands, the applications of these ligands as MTAs and ADCs in cancer therapy.
Conclusion: The maytansine site binding agents are powerful MTAs for cancer chemotherapy.
The maytansine site ligands-based ADCs are used in clinic or under clinical trials as cancer targeted
therapy to improve their selectivity and to reduce their side effects. Further improvements
in the delivery efficiency of the ADCs will benefit the patients in cancer targeted therapy.