SYNTHESIS AND BIOLOGICAL EVALUATION OF RADIOLABELLED BLOOD–BRAIN BARRIER SHUTTLE PEPTIDES
Within the framework of a collaborative project with Instituto de Medicina Molecular, Faculdade de Medicina, Univ. Lisboa and Faculdade de Medicina Veterinária, Univ. Lisboa, whose main goal is the development of novel trans-blood brain barrier (BBB) peptide vectors, we have prepared a family of short peptide conjugates that were labelled with the radiometals 99mTc and 67Ga. The final radiopeptides were tested both in vitro (BBB in vitro translocation model) and in vivo (healthy mice). One of the peptides, named PepH3, displayed promising brain penetration, turning it into a very promising candidate to be used as a peptide shuttle to take cargo in and out of the brain.
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Neves, V. et al. (2017) Novel Peptides Derived from Dengue Virus Capsid Protein Translocate Reversibly the Blood–Brain Barrier through a Receptor-Free Mechanism, ACS Chem. Biol., 12, 1257–1268, DOI: 10.1021/acschembio.7b00087.