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Peptide–PNA Conjugates: Targeted Transport of Antisense Therapeutics into Tumors
Author(s) -
Mier Walter,
Eritja Ramon,
Mohammed Ashour,
Haberkorn Uwe,
Eisenhut Michael
Publication year - 2003
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200219978
Subject(s) - somatostatin receptor , peptide , oligonucleotide , chemistry , internalization , somatostatin , in vivo , receptor , conjugate , cancer research , in vitro , biochemistry , biology , dna , mathematical analysis , mathematics , microbiology and biotechnology , neuroscience
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.