(111)In- and (203)Pb-Labeled Cyclic RGD Peptide Conjugate as an α(v)β(3) Integrin-Binding Radiotracer.
(111)In- and (203)Pb-Labeled Cyclic RGD Peptide Conjugate as an α(v)β(3) Integrin-Binding Radiotracer.
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(111)In 和 (203)Pb 标记的环状 RGD 肽缀合物作为 α(v)β(3) 整合素结合放射性示踪剂。
DOI:
10.1002/jlcr.2965
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发表时间:
2012
影响因子:
1.8
通讯作者:
Brechbiel,MartinW
中科院分区:
文献类型:
--
作者:
Nwe,Kido;Kim,Young-Seung;Milenic,DianeE;Baidoo,KwamenaE;Brechbiel,MartinW
Methodology for site‐specific modification and chelate conjugation of a cyclic arginine‐glycine‐aspartic acid (cRGD) peptide for the preparation of a radiotracer molecular imaging agent suitable for detecting αvβ3integrin is described. The method involves functionalizing the peptide with an aldehyde moiety and conjugation to a 1,4,7,10‐tetraazacyclododecane‐N,N′,N″,N‴‐tetraacetic acid derivative that possesses an aldehyde reactive aminooxy group. The binding assay of the111In‐labeled peptide conjugate with αvβ3integrin showed 60% bound when four equivalents of the integrin was added, a reasonable binding affinity for a monovalent modified RGD peptide.