Conjugate

Oligonucleotide Conjugate Discovery

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%.

Peptide Oligonucleotide Conjugate (POC)

Our Unique ‘One-Stop’ POC Synthesis Services

• ‘One-stop’ POC synthesis with 10+ years of experience in both oligonucleotide and peptide
• 80+ peptides, lipids, PEG linkers — readily available for conjugation chemistry
• ‘Custom-tailored’ design of linker / conjugation chemistry including dual conjugation chemistry

Learn more about our peptide platform.