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PMID:20393565
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| Citation |
Chen, L, Yang, S, Jakoncic, J, Zhang, JJ and Huang, XY (2010) Migrastatin analogues target fascin to block tumour metastasis. Nature 464:1062-6 |
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| Abstract |
Tumour metastasis is the primary cause of death of cancer patients. Development of new therapeutics preventing tumour metastasis is urgently needed. Migrastatin is a natural product secreted by Streptomyces, and synthesized migrastatin analogues such as macroketone are potent inhibitors of metastatic tumour cell migration, invasion and metastasis. Here we show that these migrastatin analogues target the actin-bundling protein fascin to inhibit its activity. X-ray crystal structural studies reveal that migrastatin analogues bind to one of the actin-binding sites on fascin. Our data demonstrate that actin cytoskeletal proteins such as fascin can be explored as new molecular targets for cancer treatment, in a similar manner to the microtubule protein tubulin. |
| Links |
PubMed PMC2857318 Online version:10.1038/nature08978 |
| Keywords |
Actins/metabolism; Animals; Antineoplastic Agents/chemistry; Antineoplastic Agents/metabolism; Antineoplastic Agents/pharmacology; Antineoplastic Agents/therapeutic use; Binding Sites/drug effects; Breast Neoplasms/drug therapy; Breast Neoplasms/pathology; Carrier Proteins/antagonists & inhibitors; Carrier Proteins/chemistry; Carrier Proteins/genetics; Carrier Proteins/metabolism; Cell Line, Tumor; Cell Movement/drug effects; Crystallography, X-Ray; Drug Resistance, Neoplasm/genetics; Female; Humans; Lung Neoplasms/prevention & control; Lung Neoplasms/secondary; Macrolides/chemistry; Macrolides/metabolism; Macrolides/pharmacology; Macrolides/therapeutic use; Mice; Mice, Inbred BALB C; Mice, Inbred NOD; Mice, SCID; Microfilament Proteins/antagonists & inhibitors; Microfilament Proteins/chemistry; Microfilament Proteins/genetics; Microfilament Proteins/metabolism; Models, Molecular; Mutation/genetics; Neoplasm Invasiveness/pathology; Neoplasm Invasiveness/prevention & control; Neoplasm Metastasis/drug therapy; Neoplasm Metastasis/pathology; Neoplasm Metastasis/prevention & control; Piperidones/chemistry; Piperidones/metabolism; Piperidones/pharmacology; Piperidones/therapeutic use; Protein Conformation |
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