Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
-
Susana Torres
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.
© Oldenbourg Wissenschaftsverlag
Articles in the same Issue
- Preface
- Radiolanthanides in endoradiotherapy: an overview
- Nuclear data for production of 88Y, 140Nd, 153Sm and 169Yb via novel routes
- A 140Nd/140Pr radionuclide generator based on physico-chemical transitions in 140Pr complexes after electron capture decay of 140Nd-DOTA
- Radiochemical and biological behaviour of 153Sm and 166Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle
- Biological evaluation of 153Sm and 166Ho complexes with tetraazamacrocycles containing methylcarboxylate and/or methylphosphonate pendant arms
- Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
- 177Lu-labeled-VG76e monoclonal antibody in tumor angiogenesis: A comparative study using DOTA and DTPA chelating systems
- Preclinical evaluation of somatostatin analogs bearing two macrocyclic chelators for high specific activity labeling with radiometals
Articles in the same Issue
- Preface
- Radiolanthanides in endoradiotherapy: an overview
- Nuclear data for production of 88Y, 140Nd, 153Sm and 169Yb via novel routes
- A 140Nd/140Pr radionuclide generator based on physico-chemical transitions in 140Pr complexes after electron capture decay of 140Nd-DOTA
- Radiochemical and biological behaviour of 153Sm and 166Ho complexes anchored by a novel bis(methylphosphonate) tetraazamacrocycle
- Biological evaluation of 153Sm and 166Ho complexes with tetraazamacrocycles containing methylcarboxylate and/or methylphosphonate pendant arms
- Radiolabelled 153Sm-chelates of glycoconjugates: multivalence and topology effects on the targeting of the asialoglycoprotein receptor
- 177Lu-labeled-VG76e monoclonal antibody in tumor angiogenesis: A comparative study using DOTA and DTPA chelating systems
- Preclinical evaluation of somatostatin analogs bearing two macrocyclic chelators for high specific activity labeling with radiometals
