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Synthesis, in vitro and in vivo characterization of new chelator DO3AAHA and it...
Fontes, André Filipe Gomes Soares; Ferreira, Paula M. T.; Prata, M. Isabel M.; Geraldes, Carlos F. G. C.; André, João P.
Ga(III) chelates of amphiphilic DOTA-based ligands : synthetic route and in vit...
Fontes, André Filipe Gomes Soares; Prata, M. Isabel M.; Geraldes, Carlos F. G. C.; André, João P.In this work we report a synthetic strategy of amphiphilic DOTA-based chelators bearing a variable size α-alkyl chain at one of the pendant acetate arms (from six to fourteen carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micelle concentration), their stability in blood serum and their lipophilicit...
Gallium labeled NOTA-based conjugates for peptide receptor-mediated medical ima...
Sá, Arsénio Vasconcelos de; Matias, Áurea A.; Prata, M. Isabel M.; Geraldes, Carlos F. G. C.; Ferreira, Paula M. T.; André, João P.We report a straightforward and efficient synthetic strategy for the synthesis of three model glycine-arginine-glycine-aspartic-glycine (GRGDG) conjugates based on derivatives of NOTA and of their Ga(III) complexes targeted to the integrin αѵβ₃receptor. 71Ga NMR spectroscopy showed that the Ga(III)-labeled conjugates are highly stable in aqueous solution. The 67Ga-labeled conjugates proved to have high kinetic ...
Triaza-based amphiphilic chelators : synthetic route, in vitro characterization...
Sá, Arsénio Vasconcelos de; Prata, M. Isabel M.; Geraldes, Carlos F. G. C.; André, João P.Radiogalium chelates are important for diagnostic imaging in nuclear medicine (PET and ƴ-scintigraphy). Micelles are adequate colloidal vehicles for the delivery of therapeutic and diagnostic agents to organs and tissues. In this paper we describe the synthesis and in vitro and in vivo studies of a series of micelles-forming Ga(III) chelates targeted for the liver. The amphiphilic ligands are based on NOTA (NOT...
Gallium labelled NOTA-based RGD-conjugates for targeting ανβ3 integrin receptor
Prata, M. Isabel M.; Sá, Arsénio de; Geraldes, Carlos F. G. C.; Ferreira, Paula M. T.; André, João P.; Matias, Áurea A.
Towards Targeted MRI: New MRI Contrast Agents for Sialic Acid Detection
Frullano, Luca; Rohovec, Jan; Aime, Silvio; Maschmeyer, Thomas; Prata, M. Isabel; Lima, J. J. Pedroso de; Geraldes, Carlos F. G. C.; Peters, Joop A.The detection of sialic acid in living systems is of importance for the diagnosis of several types of malignancy. We have designed and synthesized two new lanthanide ion ligands (L1 and L2) that are capable of molecular recognition of sialic acid residues. The basic structure of these ligands consists of a DTPA-bisamide (DTPA, diethylenetriamine pentaacetic acid) whose amide moieties each bear both a boronic fu...
Triethylenetetramine-N,N,N‘,N‘‘,N‘‘‘,N‘‘‘-hexaacetic Acid (TTHA) and TTHA-Bis(b...
Achour, Benbrahim; Costa, Judite; Delgado, Rita; Garrigues, Emmanuelle; Geraldes, Carlos F. G. C.; Korber, Nikolaus; Nepveu, Françoise; Prata, M. IsabelThe Ga3+ and In3+ complexes of TTHA-bis(butanamide) were characterized, including the X-ray structure of [Ga2(OH)2(ttha)][Na2(H2O)6].2H2O. Protonation studies of TTHA and TTHA-(BuA)2 were completed. Stability constants and structures in solution of the M3+ complexes (M = Al, Ga, Fe, In) were determined
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