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Chemical modification of PS-ASO therapeutics reduces cellular protein-binding and improves the therapeutic index.
Shen W, De Hoyos CL, Migawa MT, Vickers TA, Sun H, Low A, Bell TA 3rd, Rahdar M, Mukhopadhyay S, Hart CE, Bell M, Riney S, Murray SF, Greenlee S, Crooke RM, Liang XH, Seth PP, Crooke ST. Shen W, et al. Among authors: de hoyos cl. Nat Biotechnol. 2019 Jun;37(6):640-650. doi: 10.1038/s41587-019-0106-2. Epub 2019 Apr 29. Nat Biotechnol. 2019. PMID: 31036929
Site-specific replacement of phosphorothioate with alkyl phosphonate linkages enhances the therapeutic profile of gapmer ASOs by modulating interactions with cellular proteins.
Migawa MT, Shen W, Wan WB, Vasquez G, Oestergaard ME, Low A, De Hoyos CL, Gupta R, Murray S, Tanowitz M, Bell M, Nichols JG, Gaus H, Liang XH, Swayze EE, Crooke ST, Seth PP. Migawa MT, et al. Among authors: de hoyos cl. Nucleic Acids Res. 2019 Jun 20;47(11):5465-5479. doi: 10.1093/nar/gkz247. Nucleic Acids Res. 2019. PMID: 31034558 Free PMC article.
Understanding the effect of controlling phosphorothioate chirality in the DNA gap on the potency and safety of gapmer antisense oligonucleotides.
Østergaard ME, De Hoyos CL, Wan WB, Shen W, Low A, Berdeja A, Vasquez G, Murray S, Migawa MT, Liang XH, Swayze EE, Crooke ST, Seth PP. Østergaard ME, et al. Among authors: de hoyos cl. Nucleic Acids Res. 2020 Feb 28;48(4):1691-1700. doi: 10.1093/nar/gkaa031. Nucleic Acids Res. 2020. PMID: 31980820 Free PMC article.
Towards next generation antisense oligonucleotides: mesylphosphoramidate modification improves therapeutic index and duration of effect of gapmer antisense oligonucleotides.
Anderson BA, Freestone GC, Low A, De-Hoyos CL, Iii WJD, Østergaard ME, Migawa MT, Fazio M, Wan WB, Berdeja A, Scandalis E, Burel SA, Vickers TA, Crooke ST, Swayze EE, Liang X, Seth PP. Anderson BA, et al. Among authors: de hoyos cl. Nucleic Acids Res. 2021 Sep 20;49(16):9026-9041. doi: 10.1093/nar/gkab718. Nucleic Acids Res. 2021. PMID: 34417625 Free PMC article.
16 results