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

页码：2783 / 2799

页数：17

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