Synthesis of a poly(Gd(III)-DOTA)-PNA conjugate as a potential MRI contrast agent via post-synthetic click chemistry functionalization

被引:5
|
作者
Wang, Xiaoxiao [1 ]
Milne, Mark [1 ]
Martinez, Francisco [2 ]
Scholl, Timothy J. [2 ]
Hudson, Robert H. E. [1 ]
机构
[1] Univ Western Ontario, Dept Chem, 1151 Richmond St, London, ON N6A 5B7, Canada
[2] Univ Western Ontario, Robarts Res Inst, Dept Med Biophys, 1151 Richmond St, London, ON N6A 5B7, Canada
基金
加拿大自然科学与工程研究理事会;
关键词
PEPTIDE NUCLEIC-ACID; ALPHA-THIOSIALODENDRIMERS; MOLECULAR RECOGNITION; CELLULAR UPTAKE; BINDING; DENDRIMERS; DNA; PROTEIN; DESIGN; LECTIN;
D O I
10.1039/c7ra09040d
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Herein we present a method for the simultaneous, multiple conjugation of alkynyl-(Gd(III)-DOTA) moieties to a PNA oligomer possessing a domain of azide residues. This is achieved in a single Huisgen type coppercatalyzed azide alkyne cycloaddition (CuAAC) reaction after the oligomer assembly is completed. A triplex formed between the labelled PNA and riboadenylic acid, [(Gd(III)-DOTA)(4)-PNA](2):poly(rA), displayed higher relaxivities at any field strength compared to the single-stranded probe at the same concentration of Gd3+ ions as determined by nuclear magnetic resonance dispersion (NMRD) studies.
引用
收藏
页码:45222 / 45226
页数:5
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