Bioimaging and Biodistribution of the Metal Ion Controlled Self-Assembly of PYY3-36 Studied by SPECT/CT.
Bioimaging and Biodistribution of the Metal Ion Controlled Self-Assembly of PYY3-36 Studied by SPECT/CT.
Chembiochem. 2020 Jul 15;:
Authors: Kalomoiri P, Rodríguez-Rodríguez C, Sørensen KK, Bergamo M, Saatchi K, Häfeli UO, Jensen KJ
Abstract
Controlled self-assembly of peptide- and protein-based pharmaceuticals is of central importance for their mode of action and tuning of their properties. Peptide YY 3-36 (PYY 3-36 ) is a 36 amino acid peptide hormone that reduces food intake when peripherally administered. Herein, we describe the synthesis of a PYY 3-36 analogue functionalized with a metal ion binding 2,2'-bipyridine ligand which enables self-assembly through metal complexation. Upon addition of Cu(II), the bipyridine-modified PYY 3-36 peptide binds stoichiometric quantities of metal ions in solution and contributes to the organization of higher-order assemblies. In the current study, we aimed to explore the size effect of the self-assembly in vivo using non-invasive quantitative Single-Photon Emission Computed Tomography/Computed Tomography (SPECT/CT) imaging. For this purpose, bipyridine-modified PYY 3-36 was radiolabeled with a chelator holding 111 In(III), followed by the addition of Cu(II) to the bipyridine ligand. SPECT/CT imaging and biodistribution studies showed fast renal clearance and accumulation in the kidney cortex. The radiolabeled bipyridyl-PYY 3-36 conjugates with and without Cu(II) presented a slightly slower...
Source: Chembiochem - Category: Biochemistry Authors: Kalomoiri P, Rodríguez-Rodríguez C, Sørensen KK, Bergamo M, Saatchi K, Häfeli UO, Jensen KJ Tags: Chembiochem Source Type: research