J Med Chem. 2010 Jul 22;53(14):5352-5.

Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.

Karlberg T, Markova N, Johansson I, Hammarström M, Schütz P, Weigelt J, Schüler H.

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Structural Genomics Consortium, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, S-17177 Stockholm, Sweden.

Abstract

We report two crystal structures of the PARP domain of human tankyrase-2 (TNKS2). Tankyrases are involved in fundamental cellular processes such as telomere homeostasis and Wnt signaling. The complex of TNKS2 with the potent inhibitor XAV939 provides insights into the molecular basis of the strong interaction and suggests routes for further development of tankyrase inhibitors.

PMID:: 20565110; [PubMed - indexed for MEDLINE]

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Structures reported by this article

Human Tankyrase 2 - Catalytic Parp Domain In Complex With An Inhibitor Xav939

PDB: 3KR8

Source: Homo sapiens

Method: X-Ray Diffraction

Resolution: 2.1 Å

See all 2 structures...

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