Difference: JieZhengAbstract (1 vs. 2)

Revision 222 Jun 2010 - Main.DavidCowburn

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META TOPICPARENT name="InterfaceOfChemicalAndStructuralBiology"
Structure-based Investigation of Wnt Signaling Inhibitors

Jie Zheng

Department of Structural Biology, St. Jude Children’s Research Hospital, Memphis, TN 38105

Jie.Zheng@stjude.org

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META TOPICPARENT name="Staffarchive.InterfaceOfChemicalAndStructuralBiology"
Structure-based Investigation of Wnt Signaling Inhibitors

Jie Zheng

Department of Structural Biology, St. Jude Children's Research Hospital, Memphis, TN 38105

Jie.Zheng@stjude.org

Because of advances in technology, it is now possible to identify small molecules that can block a specific protein's active site by screening an extensive small-molecule database in silico. In this reported study, we focused on identifying inhibitors of the Wnt signaling pathway. Through structure-based virtual ligand screening and NMR spectroscopy, several drug-like compounds have been identified and those compounds have been shown to be able to disrupt the protein-protein interaction events at different points of the Wnt signaling pathway with low micromolar affinities. Wnt signaling plays a critical role in embryonic development and in the regulation of cell growth. Inappropriate activation of Wnt signaling has been implicated in cancers and other human diseases. Therefore, the inhibitors we obtained will be helpful in formulating rational approaches to the development of novel pharmaceutical agents that can interfere with specific Wnt signal events that contribute to human diseases.

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<		Because of advances in technology, it is now possible to identify small molecules that can block a specific protein’s active site by screening an extensive small-molecule database in silico. In this reported study, we focused on identifying inhibitors of the Wnt signaling pathway. Through structure-based virtual ligand screening and NMR spectroscopy, several drug-like compounds have been identified and those compounds have been shown to be able to disrupt the protein-protein interaction events at different points of the Wnt signaling pathway with low micromolar affinities. Wnt signaling plays a critical role in embryonic development and in the regulation of cell growth. Inappropriate activation of Wnt signaling has been implicated in cancers and other human diseases. Therefore, the inhibitors we obtained will be helpful in formulating rational approaches to the development of novel pharmaceutical agents that can interfere with specific Wnt signal events that contribute to human diseases.

Revision 127 Apr 2006 - Main.DavidCowburn

 
META TOPICPARENT name="InterfaceOfChemicalAndStructuralBiology"
Structure-based Investigation of Wnt Signaling Inhibitors

Jie Zheng

Department of Structural Biology, St. Jude Children’s Research Hospital, Memphis, TN 38105

Jie.Zheng@stjude.org

Because of advances in technology, it is now possible to identify small molecules that can block a specific protein’s active site by screening an extensive small-molecule database in silico. In this reported study, we focused on identifying inhibitors of the Wnt signaling pathway. Through structure-based virtual ligand screening and NMR spectroscopy, several drug-like compounds have been identified and those compounds have been shown to be able to disrupt the protein-protein interaction events at different points of the Wnt signaling pathway with low micromolar affinities. Wnt signaling plays a critical role in embryonic development and in the regulation of cell growth. Inappropriate activation of Wnt signaling has been implicated in cancers and other human diseases. Therefore, the inhibitors we obtained will be helpful in formulating rational approaches to the development of novel pharmaceutical agents that can interfere with specific Wnt signal events that contribute to human diseases.

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