Microtubule stabilising agents for cancer chemotherapy.
BACKGROUND
Microtubules are very important targets for cancer chemotherapy. During the past 15 years, three structurally diverse classes of microtubule stabilising agents (MSAs), namely, taxanes, epothilones and discodermolides, have been approved as anticancer agents or subjected to clinical trials, and many novel MSAs have also been identified.


OBJECTIVE
This review focuses on recent advances in the use of taxanes, epothilones and discodermolides, as well as some recently described natural product based MSAs.


METHODS
Data were identified through the search of PubMed for research articles and reviews, the website of European patents ( http://ep.espacenet.com ) and US patents ( www.uspto.gov ) for patents up to October 2008. Only well-established MSAs are mentioned in this review.


CONCLUSIONS
Great advances have been made in the application of MSAs in antitumour clinical practice and drug discovery. Many structure-activity relationship studies of MSAs as novel anticancer drugs have been conducted in recent years. To enhance the efficacy of MSAs as clinically useful therapeutics, numerous efforts have been made in combination chemotherapy regimens and include: i) the combination of structurally different MSAs, ii) combination of MSAs with other classes of anticancer agent with a different mechanism of action and iii) novel ways of administrating well-established MSAs.
Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Peking Union Medical College), Ministry of Education, Beijing, China.
Ying
Y
Zhao
Wei-Shuo
WS
Fang
Klaus
K
Pors
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000494:pharmacology; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy* / Q000503:physiopathology; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D050257:Tubulin Modulators / Q000494:pharmacology*
D000970:Antineoplastic Agents; D050257:Tubulin Modulators