442663-72-1Relevant articles and documents
In vitro and in vivo evaluations of THAM derived telomers bearing RGD and Ara-C for tumour neovasculature targeting
Jasseron,Contino-Pepin,Maurizis,Rapp,Pucci
, p. 825 - 836 (2003)
As an approach to the development of specific drug delivery systems, a new class of low macromolecular carriers called 'telomers' endowed with an antitumour agent, such as arabinofuranosylcytosine (Ara-C), RGDSK peptidic sequences, as tumour targeting moieties, and tyrosine groups labelled with 125I atoms allowing the in vivo scintigraphic follow up, were synthesized. Their tumour targeting ability was assessed in vivo in mice bearing a murine B16 melanoma. The biological results showed that the presence of RGDSK sequences onto the macromolecules leads to the selective targeting and the accumulation of telomers within the vascularized zone of the tumour. Moreover, such compounds exhibited in vitro a better IC50 (0.015 μM) than pure Ara-C and in vivo an oncostatic index higher than 160%.
Synthesis and preliminary biological assessments of RGD bearing biocompatible telomers
Jasseron, Sylvain,Contino-Pepin, Christiane,Maurizis, Jean Claude,Rapp, Maryse,Pucci, Bernard
, p. 1067 - 1070 (2002)
Work reported herein deals with the synthesis and preliminary biological assessments of a new class of biocompatible telomeric carriers bearing peptidic RGDSK sequences as tumor cell targeting and tyrosine moieties labelled with 125I as in vivo probe. The radioactivity levels obtained in several tissues, after the intravenous injections of these telomers in mice bearing grafted B16 syngenic melanoma showed that the addition of a RGD residue to a telomeric structure confers it an increased affinity for the highly vascularized zone surrounding the tumor.
