title: Clearance of the intracellular high level of the tau protein directed by an artificial synthetic hydrolase.
abstract: Promoting clearance of intracellular excessive tau is a potential therapeutic strategy for treating Alzheimer's disease. In this work, we designed and synthesized a cyclen-hybrid artificial 'hydrolase' I1-Cu(II) to cleave tau in vitro. Furthermore, a cell-permeable 'hydrolase' I2-Cu(II), derived from I1-Cu(II), was also synthesized to cleave intracellular tau proteins.
authors.affiliation: Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084, China. chen-yx@mail.tsinghua.edu.cn liym@mail.tsinghua.edu.cn.
authors.forename: Ting-Ting
authors.initials: TT
authors.lastname: Chu
authors.forename: Qian-Qian
authors.initials: QQ
authors.lastname: Li
authors.forename: Tian
authors.initials: T
authors.lastname: Qiu
authors.forename: Zhan-Yi
authors.initials: ZY
authors.lastname: Sun
authors.forename: Zhi-Wen
authors.initials: ZW
authors.lastname: Hu
authors.forename: Yong-Xiang
authors.initials: YX
authors.lastname: Chen
authors.forename: Yu-Fen
authors.initials: YF
authors.lastname: Zhao
authors.forename: Yan-Mei
authors.initials: YM
authors.lastname: Li
mesh_terms: D000544:Alzheimer Disease / Q000628:therapy; D003300:Copper / Q000737:chemistry; D000080027:Cyclams; D015195:Drug Design; D006571:Heterocyclic Compounds / Q000138:chemical synthesis; D006867:Hydrolases / Q000138:chemical synthesis*; D015394:Molecular Structure; D066263:Protein Aggregation, Pathological / Q000517:prevention & control*; D011994:Recombinant Proteins / Q000235:genetics / Q000378:metabolism; D016875:tau Proteins / Q000737:chemistry*
chemical_list: D000080027:Cyclams; D006571:Heterocyclic Compounds; D011994:Recombinant Proteins; D016875:tau Proteins; D003300:Copper; C038072:cyclen; D006867:Hydrolases