Oligonucleotide Chemical Modification Services
In the last three decades, oligonucleotides have been extensively studied as probes, molecular ligands, and even catalysts in therapeutics and diagnostics[1]. As of January 2020, ten oligonucleotide drugs have received FDA approval (Fig. 1). However, a major barrier to the widespread use of oligonucleotide therapies has been the difficulty in delivering them effectively to target organs and tissues. To overcome this shortcoming, chemical modification has become the most commonly used strategy[2].
Fig. 1. Chemistry of FDA-approved oligonucleotide drugs[2]
The Chemistry of Modified Oligos
Chemical modification of oligonucleotides can improve nucleic acid drug delivery to improve their drug-like properties, covalent conjugation to cell-targeting or cell-penetrating moieties and nanoparticle formulation. These chemical modifications include, for example, phosphorylation, biotin labeling, digoxigenin labeling, amino modification, Thiol, Spacer, Phosphorthioate, DeoxyUridine, (dU), deoxyinosine (dI), etc.
Our Oligonucleotide Chemical Modification Services:
As a professional nucleic acid drug CRO, we can provide comprehensive oligonucleotide modification and synthesis services. Before delivering the products to you, we make sure that all our products pass a strict double QC (quality and HPLC) inspection.
Advantages:
- Extensive experience
- Large-scale production: we can synthesize oligos on the 0.2 μmol, 1.0 μmol, 15 μmol, and 30 μmol scales.
- High purity: we usually purify oligos by HPLC.
- Fast delivery: deliver within 2 weeks
- Special modifications available: if any items are not included in the table below, please send us an inquiry.
- Reports: We provide reports containing O.D. values, nmol, M.V. and TM of oligonucleotides.
- Competitive pricing
We offer a wide range of modifications. We can also provide some special modifications (please contact us to inquire). Below is a list of the most frequently requested modifications.
5' -Modifications:
| 5' Amino linker C6 | 5' Amino linker C12 | 5' Phosphorylation | 5' Thiol-C6 S-S | 5' Biotin |
| 5' Dual-Biotin | 5' Digoxigenin | 5' FAM | 5' HEX | 5' TET |
| 5' JOE | 5' ROX | 5' TAMRA | 5' CY3 | 5' CY5 |
3'-Modifications:
| 3' Amino linker C7 | 3' Phosphorylation | 3' Thiol-C3 S-S | 3' Biotin | 3' Biotin TEG |
| 3' Digoxigenin | 3' FAM | 3' Dabcyl | 3' BHQ1 | 3' BHQ2 |
| 3' JOE | 3' ROX | 3' TAMRA | 3' CY3 | 3' CY5 |
Dual-Label Modifications:
| 5'-FAM,3'-DABCYL | 5'-TET,3'-DABCYL | 5'-TET,3'-BHQ1 | 5'-HEX,3'-DABCYL | 5'-TET,3'-BHQ1 |
| 5'-HEX,3'-DABCYL | 5'-JOE,3'-DABCYL | 5'TAMRA,3'-DABCYL | 5'TAMRA,3'-BHQ2 | 5'-CY5,3'-DABCYL |
| 5'-JOE,3'-BHQ1 | 5'-JOE,3'-TAMRA | 5'-FAM,3'-BHQ1 | 5'-FAM,3'-TAMRA | 5'-CY3,3'-BHQ2 |
| 5'-CY3,3'-DABCYL | 5'-CY5,3'-BHQ2 | 5'-CY5,3'-BHQ3 | 5'-ROX,3'-BHQ2 |
Other Modifications:
| dU (DeoxyUridine) | dI (DeoxyInosine) | Methyl dC | 5-Br-dU,Bromo | Spacer C3 |
| Spacer C12 | Spacer C9 | Spacer 18 | dSpacer | 2'-O-methoxyethyl-modified ribose |
| Octanediol |
Creative Biolabs can supply professional customized services on chemical modifications of nucleic acid drugs and support your research and technology applications. Please contact us to learn more.
References
- Steven Ochoa, Valeria T. Milam, Luigi A. Agrofoglio, Academic Editor, Vincent Roy, Academic Editor, and Cyril Nicolas, Academic Editor. Modified Nucleic Acids: Expanding the Capabilities of Functional Oligonucleotides. Molecules.25(20): 4659. 2020
- Thomas C. Roberts, Robert Langer, Matthew J. A. Wood.Advances in oligonucleotide drug delivery. Nature Reviews Drug Discovery. 19, pages 673–694. 2020
*For Research Use Only. Not for use in diagnostic procedures.