Synthesis and preclinical evaluation of a Zr-labelled human single chain antibody for non-invasive detection of hepatic myofibroblasts in acute liver injury.

Synaptophysin is expressed on fibrogenic hepatic myofibroblasts. C1-3 is a single chain human antibody (scAb) that binds specifically to synaptophysin on hepatic myofibroblasts, providing a targeting vector for novel in vivo imaging agents of chronic liver disease. C1-3 and a negative control scAb, CSBD9, were radiolabelled with zirconium-89 via desferrioxamine chelation to enable non-invasive molecular imaging with positron emission tomography (PET).

The influence of degree of labelling upon cellular internalisation of antibody-cell penetrating peptide conjugates.

Antibody-based agents are increasingly used as therapeutics and imaging agents, yet are generally restricted to cell surface targets due to inefficient cellular internalisation and endosomal entrapment. Enhanced cell membrane translocation of antibodies can be achieved by the covalent attachment of cell-penetrating peptides, including the HIV-1-derived transactivator of transcription (TAT) peptide. This study evaluated the cellular internalisation properties of five anti-HER2 Herceptin-TAT conjugates with degrees of TAT labelling (DOL) ranging from one to five.