111In-and 203Pb-labeled cyclic arginine-glycine-aspartic acid peptide conjugate as an av ss 3 integrin-binding radiotracer

作者：Nwe Kido; Kim Young Seung; Milenic Diane E; Baidoo Kwamena E; Brechbiel Martin W^*

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2012, 55(11): 423-426.

DOI：10.1002/jlcr.2965

• click chemistry
• aminooxy DOTA
• RGD peptide
• 203Pb

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 av beta 3 integrin 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 the 111In-labeled peptide conjugate with av beta 3 integrin showed 60% bound when four equivalents of the integrin was added, a reasonable binding affinity for a monovalent modified RGD peptide.

• 出版日期2012-9