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Susana Torres, Jose A. Martins, João P. André, Maria Neves, Ana C. Santos, Maria I. M. Prata, Carlos F. G. C. Geraldes
Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
Keywords: Asialoglycoprotein receptor, Liver targeting, Lectins, Glycoconjugates, Lanthanide(III) chelates
In this paper we report and discuss the biodistribution studies with Wistar rats of a series of 153Sm(III)-glycoconjugates, based on DO3A and DO2A( cis) scaffolds (DO3A=1,4,7-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane; DO2A(cis)=1,4-bis(carboxymethyl)-1,4,7,10-tetraazacyclododecane). The effects of changing the sugar type (galactose, lactose and glucose), valency (mono and divalent) and topology on the targeting ability of the liver asialoglycoprotein receptor (ASGPR) are evaluated. Divalent glycoconjugates with different topologies were generated by a pendant glycodendrimeric (generation 1) architecture on a DO3A scaffold and by a linear DO2A(cis)-bis derivative. The results show that the galactose conjugates are more target efficient than the lactose analogues, while the glucose conjugates have no liver targeting ability. Divalent galactose conjugates are more efficiently targeted to the liver than the monovalent ones, while the dendrimeric topology of DO3A-Gal2 has higher targeting efficiency than that of the DO2A(cis )-Gal2.
Radiochimica Acta, Oldenbourg Wissenschaftsverlag
Print ISSN: 0033-8230
Volume: 95, 06/2007
Pages: 343 - 349