Structural Basis for the Interaction between Tankyrase-2 and a Potent Wnt-Signaling Inhibitor

被引:106
作者
Karlberg, Tobias [1 ]
Markova, Natalia [1 ,2 ]
Johansson, Ida [1 ]
Hammarstrom, Martin [1 ]
Schutz, Patrick [1 ]
Weigelt, Johan [1 ]
Schuler, Herwig [1 ]
机构
[1] Karolinska Inst, Dept Med Biochem & Biophys, Struct Genom Consortium, S-17177 Stockholm, Sweden
[2] iNovacia AB, S-11251 Stockholm, Sweden
基金
英国惠康基金; 加拿大创新基金会;
关键词
POLY(ADP-RIBOSE) POLYMERASE; CATALYTIC DOMAIN; BINDING; CANCER;
D O I
10.1021/jm100249w
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:5352 / 5355
页数:4
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