Synthesis and biological evaluation of immunoconjugates of adriamycin and a human IgM linked by poly[N5-(2-hydroxyethyl)-l-glutamine

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Hoes, C.J.T. and Ankone, M.J.K. and Grootoonk, J. and Feijen, J. and Struik, E. van der and Doornmalen, A. van and Pham, D. and Man, A. de and Ettekoven, A. van and Schlachter, I. and Boon, P.J. and Kaspersen, F. and Bos, E.S. (1996) Synthesis and biological evaluation of immunoconjugates of adriamycin and a human IgM linked by poly[N5-(2-hydroxyethyl)-l-glutamine. Journal of Controlled Release, 38 (2-3). pp. 245-266. ISSN 0168-3659

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Abstract:The synthesis and purification of radiolabelled immunoconjugates, composed of a human IgM monoclonal antibody (IgM 16.88) directed against an intracellular tumour-associated antigen, the drug carrier poly[N5-(2-hydroxyethyl)--glutamine] (PHEG) and the cytostatic drug adriamycin (ADR) are described. The immunoconjugates were constructed to allow selective release of ADR in the putatively acidic environment of the tumour through a novel acid-labile maleamic acid linker. The conjugate of PHEG and the acid-labile ADR derivative effectively released ADR in cytotoxic amounts at a pH of 6.0 as judged from incubation in buffer and from inhibition of the growth of HT-29 colon tumour cells in vitro. Immunoconjugates were prepared by coupling of PHEG-ADR having a hydrolytically stable amide bond with 131I-labelled antibody through thioether bond formation involving a single thiol group at the C-terminus of the polymer chain and maleimido groups introduced onto the
Item Type:Article
Copyright:© 1996 Elsevier Science
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Science and Technology (TNW)
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Link to this item:http://purl.utwente.nl/publications/9853
Official URL:http://dx.doi.org/10.1016/0168-3659(95)00126-3
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