Recent advances in the structure-based rational design of TNKSIs

被引：22
|
作者：
Zhan, Peng [1 ,2 ]
Song, Yu'ning [1 ]
Itoh, Yukihiro [2 ]
Suzuki, Takayoshi [2 ]
Liu, Xinyong [1 ]
机构：
[1] Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, Key Lab Chem Bio,Minist Educ, Jinan 250012, Shandong, Peoples R China
[2] Kyoto Prefectural Univ Med, Grad Sch Med Sci, Sakyo Ku, Kyoto 6060823, Japan
来源：
MOLECULAR BIOSYSTEMS | 2014年 / 10卷 / 11期
基金：
中国国家自然科学基金; 高等学校博士学科点专项科研基金; 中国博士后科学基金;
关键词：
SMALL-MOLECULE INHIBITORS; LIGAND EFFICIENCY; WNT PATHWAY; TANKYRASE; POTENT; DISCOVERY; PARP; TARGETS; POCKET; OXAZOLIDINONES;
D O I：
10.1039/c4mb00385c
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Human tankyrases 1 and 2 (TNKS1/2) are attractive pharmacological biotargets, especially for the treatment of specific types of cancer. This article provides a fairly comprehensive overview of the structural biology of the TNKS-inhibitor complex and the current medicinal chemistry strategies being used in the structure-based rational design of tankyrase-specific inhibitors.
引用
收藏
页码：2783 / 2799
页数：17
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