Premium
111 In‐ and 203 Pb‐labeled cyclic arginine‐glycine‐aspartic acid peptide conjugate as an α v β 3 integrin‐binding radiotracer
Author(s) -
Nwe Kido,
Kim YoungSeung,
Milenic Diane E.,
Baidoo Kwamena E.,
Brechbiel Martin W.
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2965
Subject(s) - conjugate , peptide , glycine , chemistry , arginine , aspartic acid , moiety , integrin , stereochemistry , amino acid , chelation , aldehyde , cyclic peptide , dota , combinatorial chemistry , biochemistry , organic chemistry , mathematical analysis , mathematics , catalysis , cell
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 α v β 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 111 In‐labeled peptide conjugate with α v β 3 integrin showed 60% bound when four equivalents of the integrin was added, a reasonable binding affinity for a monovalent modified RGD peptide.