Microtubules are key components of the cytoskeletal structure of eukaryotic cells. Composed of alpha- and beta- tubulin sub-units, microtubules are dynamic entities with pivotal cellular roles (e.g. division and mitosis). Because of these unique characteristics, the first microtubule-based anti-cancer drugs have been described in the early 70’s. Here, we will review the 6 most popular small compounds active on tubulin polymerization and microtubules which are regularly used in today’s microtubule-centred in vitro assays.
Microtubule depolymerizing/inhibitor agents
- Ansamitocin P3 (CAS# 66547-09-9) is a fungal metabolite from Actinosynnema pretiosum. Ansamitocin P3 is a maytansine analog which displays potent cytotoxicity against various human tumor cell lines. Maytansine (and analogs) cause extensive disassembly of microtubules by interacting with tubulin molecules.
- Colchicine (CAS# 64-86-8) is a naturally occurring alkaloid acting as an antimitotic agent. It binds to tubulin and depolymerizes microtubules. Colchine has been shown to induce apoptosis in a variety of cell lines.
- Nocodazole (CAS# 31430-18-9) is an anti-mitotic agent (cell cycle arrest at G2/M phase) disrupting microtubules by binding to ß-tubulin and thereby inhibiting microtubule dynamics. It causes a disruption of mitotic spindle function and fragmentation of the Golgi complex. Nocodazole also activates the JNK/SAPK signaling pathway and induces apoptosis in a variety of cell lines.
- Vinblastine sulfate (CAS# 143-67-9) is a semi-synthetic alkaloidal anticancer agent. It induces cell cycle arrest at G2/M phase by inhibiting mitotic spindle formation. Vinblastine sulfate inhibits normal microtubule assembly and induces aberant tubulin polymerization causing apoptosis. This compound also inhibits autophagosome maturation.
Taxol chemical structure (33069-62-4).
Microtubule stabilizing agents
- Docetaxel (CAS# 114977-28-5) is an antimitotic chemotherapeutic with reversible high-affinity binding to microtubules. It induces apoptosis in a variety of cancer cell lines. Nevertheless, tumor cells can quickly develop resistance to docetaxel via several mechanisms.
- Taxol (CAS# 33069-62-4) is a cancer chemotherapeutic agent (breast, non-small cell lung and ovarian cancers). It acts as a promoter of tubulin polymerization by stabilizing microtubules in vitro and in vivo leading to arrest of cells in the G2 and M phase of the cell cycle.
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