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Preclinical and Clinical Advances of GalNAc-Decorated Nucleic Acid Therapeutics
Open accessAbstract
A main challenge in realizing the full potential of nucleic acid therapeutics is efficient delivery of them into targeted tissues and cells. N-acetylgalactosamine (GalNAc) is a well-defined liver-targeted moiety benefiting from its high affinity with asialoglycoprotein receptor (ASGPR). By conjugating it directly to the oligonucleotides or decorating it to a certain delivery system as a targeting moiety, GalNAc has achieved compelling successes in the development of nucleic acid therapeutics in recent years. Several oligonucleotide modalities are undergoing pivotal clinical studies, followed by a blooming pipeline in the preclinical stage. This review covers the progress of GalNAc-decorated oligonucleotide drugs, including siRNAs, anti-miRs, and ASOs, which provides a panorama for this field.
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Cites
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Cited by
Therapeutic siRNA: state of the art
Hu, B., Zhong, L., Weng, Y., Peng, L., Huang, Y., Zhao, Y., & Liang, X.-J. (2020) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-0207-x · Cited by 1,586
Self-citationGalNAc-siRNA conjugates: leading the way for delivery of RNAi therapeutics
Springer, A. D., & Dowdy, S. F. (2018) · Nucleic Acid Therapeutics · doi:10.1089/nat.2018.0736 · Cited by 711
Chemistry, mechanism and clinical status of antisense oligonucleotides and duplex RNAs
Shen, X., & Corey, D. R. (2018) · Nucleic Acids Research · doi:10.1093/nar/gkx1239 · Cited by 632
Delivery of oligonucleotides to the liver with GalNAc: From research to registered therapeutic drug.
Debacker, A. J., Voutila, J., Catley, M., Blakey, D., & Habib, N. (2020) · Molecular Therapy · doi:10.1016/j.ymthe.2020.06.015 · Cited by 424
Trials and Tribulations of MicroRNA Therapeutics
Seyhan, A. A. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25031469 · Cited by 381
Metadata
- Authors
- Huang, Y.
- Venue
- Molecular Therapy - Nucleic Acids
- Publisher
- Elsevier BV
- Published
- 2017-03
- Volume
- 6
- Pages
- 116-132
- ISSN
- 2162-2531 (ISSN-L)
- OpenAlex
- W2563642244
- Cited by
- 291
- References
- 6
- FWCI
- 14.60
- Type
- journal article
- Language
- en
- Open access
- gold
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