Single-chain antibody conjugated to a cage amine chelator and labeled with positron-emitting copper-64 for diagnostic imaging of activated platelets

Mol Pharm. 2014 Aug 4;11(8):2855-63. doi: 10.1021/mp500209a. Epub 2014 Jul 14.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Carotid Arteries / physiopathology
  • Chelating Agents / chemistry*
  • Copper / chemistry
  • Copper Radioisotopes / chemistry
  • Diagnostic Imaging
  • Disease Models, Animal
  • Flow Cytometry
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Inflammation
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Mice
  • Mice, Inbred BALB C
  • Platelet Activation
  • Positron-Emission Tomography*
  • Radiopharmaceuticals
  • Single-Chain Antibodies / chemistry*
  • Thrombosis / diagnosis
  • X-Ray Microtomography

Substances

  • Chelating Agents
  • Copper Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Ligands
  • Radiopharmaceuticals
  • Single-Chain Antibodies
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Copper