| Literature DB >> 24999533 |
Karen Alt1, Brett M Paterson, Katie Ardipradja, Christine Schieber, Gojko Buncic, Bock Lim, Stan S Poniger, Bjoern Jakoby, Xiaowei Wang, Graeme J O'Keefe, Henri J Tochon-Danguy, Andrew M Scott, Uwe Ackermann, Karlheinz Peter, Paul S Donnelly, Christoph E Hagemeyer.
Abstract
Imaging of activated platelets using an activation specific anti-GPIIb/IIIa integrin single-chain antibody (scFvanti-LIBS) conjugated to a positron emitting copper-64 complex of a cage amine sarcophagine chelator (MeCOSar) is reported. This tracer was compared in vitro to a (64)Cu(II) complex of the scFv conjugated to another commonly used macrocycle, DOTA. The scFvanti-LIBS-MeCOSar conjugate was radiolabeled with (64)Cu(II) rapidly under mild conditions and with higher specific activity than scFvanti-LIBS-DOTA. The utility of scFvanti-LIBS-MeCOSar as a diagnostic agent was assessed in vivo in a mouse model of acute thrombosis. The uptake of scFvanti-LIBS-(64)CuMeCOSar in the injured vessel was significantly higher than the noninjured vessel. Positron emission tomography (PET) was used to show accumulation of scFvanti-LIBS-(64)CuMeCOSar with high and specific uptake in the injured vessel. ScFvanti-LIBS-(64)CuMeCOSar is an excellent tool for highly sensitive in vivo detection of activated platelets in PET and has the potential to be used for early diagnosis of acute thrombotic events.Entities:
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Year: 2014 PMID： 24999533 DOI： 10.1021/mp500209a
Source DB: PubMed Journal: Mol Pharm ISSN： 1543-8384 Impact factor: 4.939