Peptide-PNA conjugates: Targeted transport of antisense therapeutics into tumors

被引:34
作者
Mier, W
Eritja, R
Mohammed, A
Haberkorn, U
Eisenhut, M
机构
[1] Univ Klinikum Heidelberg, Radiol Klin, Abt Nukl Med, D-69120 Heidelberg, Germany
[2] CSIC, Cid, ES-08034 Barcelona, Spain
[3] Deutsch Krebsforschungszentrum, D-69120 Heidelberg, Germany
关键词
antisense agents; drug delivery; peptide nucleic acids; peptides; solid-phase synthesis;
D O I
10.1002/anie.200219978
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Tumor-specific accumulation of antisense therapeutics: The conjugation of a receptor-binding peptide allows for the first time the selective transport of oligonucleotide analogues into tumor tissue. By using the tert-butyloxycarbonyl (Boc) protecting group stratergy, hybrids of peptide nucleic acids and peptides are accessible that accumulate in tumor tissue at a tenfold higher concentration than the free peptide nucleic acid.
引用
收藏
页码:1968 / 1971
页数:4
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