title: Recent advances in the structure-based rational design of TNKSIs.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Key laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P. R. China. zhanpeng1982@sdu.edu.cn xinyongl@sdu.edu.cn.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.forename: Yu'ning
authors.initials: Y
authors.lastname: Song
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D020134:Catalytic Domain; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D015398:Signal Transduction / Q000187:drug effects; D038501:Tankyrases / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D038501:Tankyrases; C437334:TNKS2 protein, human; C418109:TNKS protein, human