Table 1 Overview of oligonucleotides used in different proof-of-concept studies. Capital letters in sequence describe LNA-modified nucleosides, small letters describe DNA nucleosides. GN: GalNAc, AmC6: amino hexylene, GBB-Am: aminopropyl glycerol based bridge, C6SH: hexylene sulfhydryl, NSP: N-succinimidyl propionate, NMM: N-methylmaleimide, NEM: N-ethylmaleimide, i: in vitro target reduction and MetID, ii: in vivo mouse PK study. Column “Study” describes the use of oligonucleotides in different studies
From: Tritium labeling of antisense oligonucleotides via different conjugation agents
ASO | Oligonucleotide sequence 5′ → 3′ | Linker | Adduct | Study |
|---|---|---|---|---|
1 | 5′-GAGttacttgccaACT-3′ | --- | --- | i, ii |
2 | 5′-GAGttacttgccaACT-3′ | 3′-GBB-Am | NSP | i |
3 | 5′-GAGttacttgccaACT-3′ | 3′-C6SH | NMM | i |
4 | 5′-GAGttacttgccaACT-3′ | 3′-C6SH | NEM | i |
5 | 5′-GN-AmC6-caGAGttacttgccaACT-3′ | --- | --- | i, ii |
6 | 5′-GN-AmC6-caGAGttacttgccaACT-3′ | 3′-C6SH | NEM | i |
7 | 5′-GAGttacttgccaACT-3′ | 3′-C6SH | [3H]-NEM | ii |
8 | 5′-GN-AmC6-caGAGttacttgccaACT-3′ | 3′-C6SH | [3H]-NEM | ii |