RNA修飾
薬物としての小分子核酸が細胞内に取り込まれ、機能を発揮するかどうかは、デリバリー方法と効率が重要な要素となります。主なデリバリーアプローチには、ヌードRNAの修飾デリバリー技術、リポソームナノデリバリー技術、小分子リガンドや抗体などを用いたコンジュゲート型デリバリーシステム、その他新しいタイプのデリバリーシステムがあります。
GenCefe Biotech は、さまざまな核酸医薬のデリバリーニーズに対応するため、RNAの修飾、ラベリング、コンジュゲーションサービス を包括的に提供しています。豊富な専門知識と革新的な技術を背景に、研究の発展を支援するパートナーとしてご活用いただけます。
RNA修飾
| Modification Type | Modifications | Modification Type | Modifications |
| Point Modification | 2'OME | Special Modifications | Cholesterol |
| dspacer | GalNAc | ||
| dI | DBCO | ||
| rI | Desthiobiotin | ||
| dU | Cy5.5 | ||
| 2'F | Cy7 | ||
| 2'MOE | Hexynyl | ||
| LNA | BHQ1 | ||
| m6A | BHQ2 | ||
| m5C | BHQ3 | ||
| m5U | MGB | ||
| End Modifications | Thiol | ATTO Series | |
| Amino Linker | Chimeric RNA | DNA\RNA | |
| Biotin | RNA\2'F\2'OME\DNA | ||
| Phosphorylation | Dual-Labeling | FAM-BHQ1 | |
| spacer C9 | FAM-TAMRA | ||
| spacer C18 | FAM-Dab | ||
| Fluorescent Labeling | FAM | TAMRA-BHQ2 | |
| HEX | CY3-BHQ2 | ||
| Cy3 | CY5.5-BHQ3 | ||
| Cy5 | CY7-BHQ3 | ||
| TET | |||
| VIC | |||
| TAMRA |
小分子核酸医薬向け修飾
Nucleic Acid Type | Chemical Modification and Fluorescent Labeling Services |
siRNA | Sugar Modification: 2'-Ome , 2'-F, etc. Backbone Modification: PS (phosphorothioate) modification, etc. E nd modification: Chol (cholesterol), Biotin, Thiol, NH 2 , etc. Fluorescent labeling: Cy3, Cy5, etc. Customized chemical modification and fluorescent labeling proposal design |
Antisense (ASO) | Sugar Modification: 2'-OMe, 2'-MOE, 2'-F, LNA, etc. Base Modification: methylated cytosine (5-Me-dC), etc. Backbone Modification: PS (phosphorothioate) modification, etc. E nd modification: Chol (cholesterol), etc. |
Aptamer | Sugar Modification: 2'-OMe, 2'-NH2, 2'-F, LNA, etc. Base Modification: methylated cytosine (5-Me-dC), etc. Backbone Modification: PS (phosphorothioate) modification, etc. E nd modification: 3'-inverted thymidine, Chol (cholesterol), Biotin, Thiol, NH 2 , fluorescent dyes, etc. |
Others | Custom chemical modification and fluorescent labeling services |
デリバリーシステムおよびコンジュゲーション
Delivery System | Features | Services |
GalNAc (N-acetylgalactosamine) | GalNAc is the targeting ligand of the sialic acid receptor (ASGPR), which is mainly expressed on the surface of hepatic parenchymal cells. The conjugate of nucleic acid and GalNAc enters the cell through endocytosis to function. | Custom GalNAc Synthesis GalNAc-siRNA Synthesis GalNAc-ASO Synthesis GalNAc-miRNA Synthesis Customized design and synthesis of GalNAc delivery proposal |
Peptide | Peptides have better membrane permeability and strong resistance to degradation. Therefore, conjugating oligonucleotides with various biological functions to peptides can not only improve the biological activity of oligonucleotides but also enhance their cell permeability. | Peptide Synthesis (drug peptides, custom peptides, RGD cyclic peptides, etc.) Peptide-siRNA Conjugation Peptide-ASO Conjugation Peptide-DNA Conjugation RGD-siRNA Conjugation |
Lipid | LNP not only prevents degradation of delivered oligonucleotides and prolongs circulation time, but also facilitates oligonucleotide uptake, enhances intracellular transport, and facilitates endosomal escape. | LNP-siRNA Conjugation LNP-ASO Conjugation |
PEG (polyethylene glycol) | The half-life of PEG-modified ASO in the body is significantly prolonged, and PEG can reduce the excretion rate of oligonucleotides and promote the uptake of nucleic acid drugs by corresponding cells. | PEG-Aptamer Conjugation PEG-siRNA Conjugation PEG-ASO Conjugation |
Others | / | Custom delivery proposal design and synthesis |
