CRGD peptide-conjugated icosahedral closo-B12(2-) core carrying multiple Gd3+-DOTA chelates for α(v)β3 integrin-targeted tumor imaging (MRI).

ABSTRACT: A vertex-differentiated icosahedral closo-B(12)(2-) core was utilized to construct a α(v)β(3) integrin receptor-targeted (via cRGD peptide) high payload MRI contrast agent (CA-12) carrying 11 copies of Gd(3+)-DOTA chelates attached to the closo-B(12)(2-) surface via suitable linkers. The resulting polyfunctional MRI contrast agent possessed a higher relaxivity value per-Gd compared to Omniscan, a small molecular contrast agent commonly used in clinical settings. The α(v)β(3) integrin receptor specificity of CA-12 was confirmed via in vitro cellular binding experiments and in vivo MRI of mice bearing human PC-3 prostate cancer xenografts. Integrin α(v)β(3)-positive MDA-MB-231 cells exhibited 300% higher uptake of CA-12 than α(v)β(3)-negative T47D cells. Serial T1-weighted MRI showed superio

SUBMITTER: Goswami LN 

PROVIDER: S-EPMC3593306 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature