Table 1.
High-throughput sequencing and activity screen data.
| Round | N40 Variable Sequence | Name (length in nucleotides) | FXIa Inhibition |
|---|---|---|---|
| 4 | GCGTCCAACACATCGTATTCAT | Apt4-1 (22) | − |
| 4 | TGGGATGGCGTGGGAGGGCTGTAGGGAGCGTTCAGTGGGT | Apt4-2 (40) | NT |
| 4 | GGGAGGGCGTGGATGGCTGGTGTGAGGTCTTGTGTTTGTT | Apt4-3 (40) | − |
| 4 | GGGAGCGTTCAGTGGGT | Apt4-4 (17) | NT |
| 4 | GCGTCCAACACATCGGATGATAT | Apt4-5 (23) | NT |
| 4 | TGCGTCCAACACATCGTATTCAT | Apt4-6 (23) | NT |
| 4 | TGGGATGGCGTGGGAGGGCTGTAGTGAGCGTTCAGTGGGT | Apt4-7 (40) | NT |
| 4 | CGTCCAACACATCGTATTCAT | Apt4-8 (21) | NT |
| 4 | CTTGCCCACTATCGACTTCACC | Apt4-9 (22) | NT |
| 4 | GCGTCCAACACATCGTAAGTA | Apt4-10 (21) | NT |
| 10 | GCGTCCAACACATCGTATTCAT | Apt10-1 (22) | − |
| 10 | CACTGCGTCCAACACATCGTATTCAT | Apt10-2 (26) | − |
| 10 | TGGGATGGCGTGGGAGGGCTGTAGGGAGCGTTCAGTGGGT | Apt10-3 (40) | − |
| 10 | TGGGATGGCGTGGGAGGGCTGTAGTGAGCGTTCAGTGGGT | Apt10-4 (40) | − |
| 10 | GGGAGGGCGTGGATGGCTGTTGTGAGGTCTTGTGTTTGTT | Apt10-5 (40) | − |
| 10 | TGGGATGGCGTGGGAGGGCTGTAGGGAGCGTTTAGTGGGT | Apt10-6 (40) | − |
| 10 | TGGGATGGCGTGGGAGGGCTGTAGTGAGCGTTCATTGGGT | Apt10-7 (40) | − |
| 10 | GGGAGGGCGTGGATGGCTGGTGTGAGGTCTTGTGTTTGTT | Apt10-8 (40) | − |
| 10 | TGGGATGGCGTGGGAGGGCTGTAGTGAGCGTTTAGTGGGT | Apt10-9 (40) | − |
| 10 | AACCTATCGGACTATTGTTAGTGATTTTTATAGTGT | Apt10-10 (36) | + |
DNA sequence of aptamers (name and length in nucleotides, column 3) isolated after 4 or 10 rounds of screening (column 1) corresponding to the N40 variable domain in the original aptamer library (5′-GAATTCTAAT ACGACTCACT ATA-N40-GCGTCCAACA CATCG-3′) is given in column 2. Whether (+) or not (−) the aptamer had inhibitory activity when introduced into FXIa-mediated amidolysis of S2366 is shown in column 4. The ten most abundant sequences obtained after Rounds 4 or 10 are shown in rank order; NT signifies not tested.