Radiolabeled DNA oligonucleotide and method of preparation

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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435 6, 435375, 514 44, 536 243, 536 2431, 536 2532, C07H 2100, C07H 2104, A61K 3170, C12N 510

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active

058213546

ABSTRACT:
The present invention relates to a radiolabeled DNA oligonucleotide, a method of preparation thereof and the therapeutic uses of this substance to prevent uncontrolled cellular proliferation. The invention also relates to devices incorporating the above radiolabeled DNA oligonucleotide for the therapeutic treatment of uncontrolled cellular proliferation. More specifically, the present invention is concerned with the prevention of restenosis by coronary delivery of radiolabeled DNA oligonucleotide at a dilatation site of an artery. This invention is also directed to a method of treatment of vascular proliferative diseases and/or other proliferative disorders such as cancer and related metastasis. More particularly, the invention relates to the preparation of DNA sequences carrying one or several radioisotopes, located within the DNA sequence, and which are able to prevent cell proliferation in vitro and, pursuant to local drug delivery, are able to prevent cell proliferation in vivo, more particularly restenosis and malignant tumors. In other words, the invention relates to the synthesis process, the stability data of the radiolabeled DNA oligonucleotide, the efficacy of the invention in vitro, in cell culture, and the in vivo delivery of the molecule.

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