Table 3Specificity and potency of human telomerase inhibition in vitro by template-targeting 2'-OMe RNA, 2'-OMOE RNA, PNA and DNA

inhibitorlength (nt) 5'-sequence-3' IC50 a refs
2'-OMe RNA 813 -CAGUUAGGGUUAG8 nM 42
2'-OMOE RNA 913-CAGUUAGGGUUAG10 nM 45
PNA 1013 -CAGTTAGGGTTAG20 nM 42
DNA 1113-CAGTTAGGGTTAGN/Db 42
2'-OMe RNA 1213-mismatch-GACUUAGAAUUAGN/D 42
2'-OMOE RNA 1313-mismatch-CAGUUAGAAUUAG>10 μM 45
2'-OMe RNA 1413-CAGUUAGGGUUAG 3 nM 42
2'-OMe RNA 1513-mismatch-CAGUUAGAAUUAG 3 mM 42
2'-OMOE RNA 1613-CAGUUAGGGUUAG 9 nM 45
2'-OMOE RNA 1713-mismatch-CAGUUAGAAUUAG >10 μM 45
2'-OMe RNA 1813-CAGUUAGGGUUAG 30 nM 42
2'-OMe RNA 1913-mismatch-CAGUUAGAAUUAG 200 nM 42
2'-OMOE RNA 2013-CAGUUAGGGUUAG 7 nM 45
2'-OMOE RNA 2113-mismatch-CAGUUAGAAUUAG 1.1 μM 45
target RNA sequence -GUCAAUCCCAAUCUGUUU41-  5'   

a IC50 values determined with the telomere repeat-amplification protocol (TRAP) at 37°C.

b N/D: not detectable. The italicized bases within the sequences represent the mismatched nucleotides. Underlined sequences have phosphorothioate linkages.

From: PNA and Oligonucleotide Inhibitors of Human Telomerase

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