3KR8

Human tankyrase 2 - catalytic PARP domain in complex with an inhibitor XAV939

Summary for 3KR8

• Entry DOI: 10.2210/pdb3kr8/pdb
• Related: 3KR7
• Descriptor: Tankyrase-2, ZINC ION, 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, ... (6 entities in total)
• Functional Keywords: catalytic fragment, parp, structural genomics, structural genomics consortium, sgc, adp-ribosylation, ank repeat, chromosomal protein, glycosyltransferase, golgi apparatus, membrane, mrna transport, nad, nuclear pore complex, nucleus, phosphorylation, protein transport, telomere, transferase, translocation, transport, wnt-signalling, xav939
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: Q9H2K2
• Total number of polymer chains: 2
• Total formula weight: 55923.41

Authors

Karlberg, T.,Schutz, P.,Arrowsmith, C.H.,Berglund, H.,Bountra, C.,Collins, R.,Edwards, A.M.,Flodin, S.,Flores, A.,Graslund, S.,Hammarstrom, M.,Johansson, A.,Johansson, I.,Kallas, A.,Kotenyova, T.,Kotzsch, A.,Kraulis, P.,Nielsen, T.K.,Moche, M.,Nordlund, P.,Nyman, T.,Persson, C.,Siponen, M.I.,Thorsell, A.G.,Tresaugues, L.,Van Den Berg, S.,Weigelt, J.,Welin, M.,Wisniewska, M.,Schuler, H.,Structural Genomics Consortium (SGC) (deposition date: 2009-11-18, release date: 2009-12-15, Last modification date: 2023-11-01)

Primary citation

Karlberg, T.,Markova, N.,Johansson, I.,Hammarstrom, M.,Schutz, P.,Weigelt, J.,Schuler, H.
Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.
J.Med.Chem., 53:5352-5355, 2010

PubMed 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.

PubMed: 20565110
DOI: 10.1021/jm100249w

Experimental method

X-RAY DIFFRACTION (2.1 Å)