Peloruside A, a novel antimitotic agent with paclitaxel-like microtubule- stabilizing activity.
Peloruside A is a novel secondary metabolite isolated from a New Zealand marine sponge, Mycale hentscheli, that has potent paclitaxel-like microtubule-stabilizing activity and is cytotoxic at nanomolar concentrations. Its 16-membered macrolide ring is similar to that of epothilone, a drug currently under clinical investigation as an anticancer agent. Like paclitaxel, peloruside A arrests cells in the G(2)-M phase of the cell cycle and induces apoptosis. The relatively simple structure of peloruside makes it suitable for the design and synthesis of analogues with improved tumor targeting and reduced tumor cross-resistance.
Hood
Kylie A
KA
School of Biological Sciences, Victoria University of Wellington, New Zealand.
West
Lyndon M
LM
Rouwé
Berber
B
Northcote
Peter T
PT
Berridge
Michael V
MV
Wakefield
St John
SJ
Miller
John H
JH
D000199:Actins / Q000378:metabolism; D000230:Adenocarcinoma / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D034261:Epothilones; D006801:Humans; D007783:Lactones / Q000737:chemistry / Q000494:pharmacology*; D008175:Lung Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D018942:Macrolides / Q000737:chemistry / Q000494:pharmacology; D008870:Microtubules / Q000187:drug effects; D017239:Paclitaxel / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D043823:Taxoids; D014404:Tubulin / Q000378:metabolism
D000199:Actins; D000970:Antineoplastic Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D034261:Epothilones; D007783:Lactones; D018942:Macrolides; D043823:Taxoids; D014404:Tubulin; C117305:laulimalide; C414085:peloruside A; D017239:Paclitaxel; C093788:epothilone B