Table 1. Inhibition of telomerase by 2′-MOE RNA and 2′-MOE RNA/DNA chimeric oligomers.
Compound | Chemistry | No. | Sequence | IC50 (µM) | |
|
|
|
|
25°C |
37°C |
3′-GAAGAGUCAAUCCCAAUCUG-5′ (RNA template) | |||||
ISIS24690 | 2′-MOE RNA | I | CAGUUAGGGUUAG | 0.03 | 0.01 |
ISIS125626 | 2′-MOE RNA | II | CAGUUAGAAUUAG (mismatch) | >10 | >10 |
ISIS125625 | 2′-MOE RNA | III | CAGUUAGGGUUAG | 0.002 | 0.009 |
ISIS125627 | 2′-MOE RNA | IV | CAGUUAGAAUUAG (mismatch) | 3.3 | 7 |
ISIS24691 | 2′-MOE RNA | V | CAGUUAGGGUUAG | 0.003 | 0.007 |
ISIS125628 | 2′-MOE RNA | VI | CAGUUAGAAUUAG (mismatch) | 0.7 | 1.1 |
ISIS113753 | 2′-MOE RNA/DNA | VII | CUUCUCAGTTAGGGTUAGAC | 0.025 | 0.02 |
ISIS113754 | 2′-MOE RNA/DNA | VIII | CUUCUCAGTTAGAATUAUAC (mismatch) | 1.0 | >5.5 |
ISIS113751 | 2′-MOE RNA/DNA | IX | CUUCUCAGTTAGGGTUAGAC | 0.002 | 0.005 |
ISIS113752 | 2′-MOE RNA/DNA | X | CUUCUCAGTTAGAATUAUAC (mismatch) | 0.004 | 0.010 |
ISIS113749 | 2′-MOE RNA/DNA | XI | CUUCUCAGTTAGGGTUAGAC | 0.006 | 0.009 |
ISIS113750 | 2′-MOE RNA/DNA | XII | CUUCUCAGTTAGAATUAUAC (mismatch) | 0.008 | 0.009 |
Underlined nucleotides have PS linkages. The italicized bases in the 2′-MOE/DNA chimera are DNA.