Title: Synthesis and cleavage experiments of oligonucleotide conjugates with a diimidazole-derived catalytic center
Authors: Verbeure, B ×
Lacey, Carl Jeff
Froeyen, Mathy
Rozenski, Jef
Herdewijn, Piet #
Issue Date: 2002
Publisher: Amer chemical soc
Series Title: Bioconjugate chemistry vol:13 issue:2 pages:333-350
Abstract: Ribonuclease mimics based on diimidazole derived constructs in combination with or without additional amino groups have been synthesized and conjugated to oligonucleotides. The imidazole moiety was used either unprotected, protected with a monomethoxytrityl group or a tert-butyloxy carbonyl group. Acylation reactions were carried out using the 3-acyl-1,3-thiazolidine-2-thione activation strategy. The peptides were coupled to the oligonucleotides with a mixture of PyBOP, DIEA an HOBt in DMF on solid support. The conjugates were purified by RP-HPLC and identified using negative ion mode mass spectrometry. Unfortunately, no cleavage of a linear RNA target under physiological conditions could be observed.
ISSN: 1043-1802
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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