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Natural Product Reports
- Source :
- Natural Product Reports
- Publication Year :
- 2014
- Publisher :
- Royal Society of Chemistry (RSC), 2014.
-
Abstract
- Zampanolide and its structural relative dactylolide are promising new tubulin-assembly agents with the potential to become new anticancer drugs. This review covers their sources and isolation, structures, anticancer potential, mechanism of action, and syntheses.<br />Covering: through January 2014 Zampanolide is a marine natural macrolide and a recent addition to the family of microtubule-stabilizing cytotoxic agents. Zampanolide exhibits unique effects on tubulin assembly and is more potent than paclitaxel against several multi-drug resistant cancer cell lines. A high-resolution crystal structure of αβ-tubulin in complex with zampanolide explains how taxane-site microtubule-stabilizing agents promote microtubule assemble and stability. This review provides an overview of current developments of zampanolide and its related but less potent analogue dactylolide, covering their natural sources and isolation, structure and conformation, cytotoxic potential, structure–activity studies, mechanism of action, and syntheses.
- Subjects :
- Bridged-Ring Compounds
Zampanolide
Paclitaxel
Stereochemistry
Antineoplastic Agents
Marine Biology
Anti-cancer drugs
010402 general chemistry
Microtubules
01 natural sciences
Biochemistry
Lactones
chemistry.chemical_compound
Tubulin
Microtubule
Drug Discovery
medicine
Cytotoxic T cell
Cytotoxic agents
Cytotoxicity
Molecular Structure
biology
010405 organic chemistry
Organic Chemistry
Dactylolide
Bridged Bicyclo Compounds, Heterocyclic
3. Good health
0104 chemical sciences
Multi-drug resistance
Chemistry
Microtubule stabilizing agents
Mechanism of action
chemistry
biology.protein
Taxoids
Macrolides
medicine.symptom
Subjects
Details
- ISSN :
- 14604752 and 02650568
- Volume :
- 31
- Database :
- OpenAIRE
- Journal :
- Nat. Prod. Rep.
- Accession number :
- edsair.doi.dedup.....b71bbe9762d000b188a1ec8a0a04e8fc