Clarenc J P, Lebleu B, Léonetti J P
Centre Nationale de la Recherche Scientifique UA1191, Université de Montpellier II Sciences et Techniques du Languedoc, France.
J Biol Chem. 1993 Mar 15;268(8):5600-4.
The intracellular fate of antisense oligodeoxyribonucleotide (oligomers) is poorly understood. Recent observations strongly suggest that after endocytosis and escape from the endocytic compartments, oligomers accumulate in the nuclei of eukaryotic cells by simple diffusion. Isolated nuclei were used to determine the number of these nuclear binding sites and their affinity for phosphodiester, phosphorothioate, and methyl-phosphonate oligomers. These cell-free assays were correlated with intact cell microinjection experiments. Great differences have been observed between these analogs. These data are helpful in understanding the fate of oligomers and the mechanism of their action and could be helpful for a more rational design of antisense molecules.
反义寡脱氧核糖核苷酸（寡聚物）在细胞内的命运目前还了解甚少。最近的观察结果有力地表明，寡聚物在通过胞吞作用进入细胞并从胞吞区室逃逸后，通过简单扩散在真核细胞的细胞核中积累。使用分离的细胞核来确定这些核结合位点的数量及其对磷酸二酯、硫代磷酸酯和甲基磷酸酯寡聚物的亲和力。这些无细胞试验与完整细胞显微注射实验相关联。已观察到这些类似物之间存在很大差异。这些数据有助于理解寡聚物的命运及其作用机制，并且可能有助于更合理地设计反义分子。
