The shape of things to come: structural and synthetic studies of taxol and related compounds.
The history of the development of Taxol (paclitaxel) as an anticancer drug is reviewed, and some aspects of the phytochemistry of Taxus species and of the medicinal chemistry of taxol are discussed. The nature of the taxol-tubulin interaction is then described, with an emphasis on studies that led to the discovery and experimental proof of the T-taxol conformation as the tubulin-binding conformation of taxol. The implications of this conformation for future drug development are also briefly covered.
Kingston
David G I
DG
Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University Blacksburg, VA 24061, USA. dkingston@vt.edu
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D009369:Neoplasms / Q000378:metabolism / Q000473:pathology; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000378:metabolism
D000970:Antineoplastic Agents; D014404:Tubulin; D017239:Paclitaxel