Oligonucleotide Conjugate Discovery
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Oligonucleotide conjugates create opportunities to deliver the oligonucleotide to a specific cell or tissue and to fine-tune ‘drug-like’ properties. However, the complexity of the conjugation chemistry presents significant challenges for drug innovators.
WuXi TIDES is well positioned to provide a one-stop solution for complex oligonucleotide-base conjugated drugs, from discovery through development to commercial manufacturing. Our strong capabilities extend to oligonucleotides, peptides, and small molecules, including ligands, toxins, linkers, lipids, PEG, and more. Supported by a wealth of experience, we offer flexible options with rapid turnaround time and comprehensive support for design and synthesis with analytical processes at any scale.
- GalNAc-Oligonucleotide
- Peptide-Oligonucleotide
- Aptamer-Oligonucleotide
- Lipid-Oligonucleotide
- Toxin/drug-Oligonucleotide
- Customized Small Molecule-Oligonucleotide
Conjugation Chemistry
- Amide Coupling
- Thiol-maleimide Addition
- Click Chemistry: CuAAC | SPAAC
- Disulfide Chemistry
- Hydrazone Chemistry
Linkers & Ligands
- 50+ modified PS/CPG resin (GalNAc, lipid/PEG amine, biotine, dye etc…)
- 100+ peptide conjugates (Cell-penetrating peptide, cyclic peptide, bicyclic peptide)
- 150+ cleavable / uncleavable linkers with maleimide, DBCO, BCN, azide, PySS, etc…
Topology
- 3'- or 5'-end conjugation
- Oligonucleotide moiety conjugates on base phosphorus backbones
- Complex dual conjugation: 3’,5’- | 3’,3’- | 5’,5’-
Case study 1: siRNA 'dual conjugation' enables fast ligand screening
‘Dual conjugation’ allows for the rapid screening of two ligands on one siRNA. By using this method, we conducted a 2-D screening to examine the affinity of two types of ligands. This approach exponentially increases the screening efficiency, enabling us to achieve lead optimization for 140 complex dual conjugates within just 4 to 6 weeks.
Case study 2: siRNA-peptide conjugation
We prepared siRNA and cyclic peptides, and performed special conjugation with the cyclic peptide after siRNA annealing. The SEC purity was well controlled, remaining above 90%, and was purified using our ultrafiltration technology.
Case study 3: siRNA-ASO conjugation
We prepared 5’ SH/N3 ASO and siRNA in house and delivered 14 conjugates within 5 weeks. The SEC purity by UPLC, was above 90%.
