3LLP

1.8 Angstrom human fascin 1 crystal structure

Summary for 3LLP

• Entry DOI: 10.2210/pdb3llp/pdb
• Descriptor: Fascin, GLYCEROL, POTASSIUM ION, ... (7 entities in total)
• Functional Keywords: beta-trefoil, actin bundling protein, cancer, metastasis, cell migration, acetylation, actin-binding, cytoplasm, phosphoprotein, protein binding
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm, cytoskeleton: Q16658
• Total number of polymer chains: 2
• Total formula weight: 110828.25

Authors

Chen, L.,Yang, S.,Jakoncic, J.,Zhang, J.J.,Huang, X.-Y. (deposition date: 2010-01-29, release date: 2010-04-07, Last modification date: 2024-02-21)

Primary citation

Chen, L.,Yang, S.,Jakoncic, J.,Zhang, J.J.,Huang, X.Y.
Migrastatin analogues target fascin to block tumour metastasis.
Nature, 464:1062-1066, 2010

PubMed 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.

PubMed: 20393565
DOI: 10.1038/nature08978

Experimental method

X-RAY DIFFRACTION (1.8 Å)