3CBY

The Dvl2 PDZ Domain in Complex with the N1 Inhibitory Peptide

Summary for 3CBY

• Entry DOI: 10.2210/pdb3cby/pdb
• Related: 3CBX 3CBZ 3CC0
• Descriptor: Dishevelled-2, 1,2-ETHANEDIOL (3 entities in total)
• Functional Keywords: pdz domain, phage derived high affinity ligand, cytoplasm, developmental protein, phosphoprotein, wnt signaling pathway, protein binding
• Biological source: Homo sapiens (Human)
• Cellular location: Cell membrane ; Peripheral membrane protein ; Cytoplasmic side : O14641
• Total number of polymer chains: 2
• Total formula weight: 23366.54

Authors

Appleton, B.A.,Wiesmann, C. (deposition date: 2008-02-23, release date: 2009-03-03, Last modification date: 2023-08-30)

Primary citation

Zhang, Y.,Appleton, B.A.,Wiesmann, C.,Lau, T.,Costa, M.,Hannoush, R.N.,Sidhu, S.S.
Inhibition of Wnt signaling by Dishevelled PDZ peptides
Nat.Chem.Biol., 5:217-219, 2009

PubMed Abstract: Dishevelled proteins are key regulators of Wnt signaling pathways that have been implicated in the progression of human cancers. We found that the binding cleft of the Dishevelled PDZ domain is more flexible than those of canonical PDZ domains and enables recognition of both C-terminal and internal peptides. These peptide ligands inhibit Wnt/beta-catenin signaling in cells, showing that Dishevelled PDZ domains are potential targets for small-molecule cancer therapeutics.

PubMed: 19252499
DOI: 10.1038/nchembio.152

Experimental method

X-RAY DIFFRACTION (1.5 Å)