3KR8

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

3KR8 の概要

• エントリーDOI: 10.2210/pdb3kr8/pdb
• 関連するPDBエントリー: 3KR7
• 分子名称: Tankyrase-2, ZINC ION, 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, ... (6 entities in total)
• 機能のキーワード: 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
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: Q9H2K2
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 55923.41

構造登録者

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) (登録日: 2009-11-18, 公開日: 2009-12-15, 最終更新日: 2023-11-01)

主引用文献

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

実験手法

X-RAY DIFFRACTION (2.1 Å)