Evidence map›Paper›PMID 27827561›Full record

ArticleNucleic acid therapeutics2017

A Novel PEGylation Method for Improving the Pharmacokinetic Properties of Anti-Interleukin-17A RNA Aptamers.

Kazuhiko Haruta, Natsuki Otaki, Masakazu Nagamine, Tomoyoshi Kayo, Asako Sasaki, Shinsuke Hiramoto, Masayuki Takahashi, Kuniyoshi Hota, Hideaki Sato, Hiroaki Yamazaki

Open access · hybridAbstract read
In one paragraph

Article in Nucleic acid therapeutics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
2.6field-weighted citation impact, top 10% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

23 citing papers in PubMed, 46 citations in OpenAlex.

  1. Review
  2. Aptamers in Osteosarcoma: New Paths for Diagnosis and Treatment.Anti-cancer agents in medicinal chemistry · 2026
    Review
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  8. Article
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  10. Review
  11. Controlling Coagulation in Blood with Red Light.Angewandte Chemie (International ed. in English) · 2021
    Article
  12. Article
  13. Article
  14. Using Aptamers as a Novel Method for Determining GnRH/LH Pulsatility.International journal of molecular sciences · 2020
    Review
  15. Review
  16. Review
  17. Review
  18. Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 1 institution in 1 country.

Kazuhiko Haruta1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Natsuki Otaki1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Masakazu Nagamine1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Tomoyoshi Kayo1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Asako Sasaki1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Shinsuke Hiramoto1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Masayuki Takahashi1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Kuniyoshi Hota1 R&D Center, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Hideaki Sato2 GeneDesign, Inc. , Osaka, Japan .
Hiroaki Yamazaki3 Prescription Products Development, Zenyaku Kogyo Co., Ltd. , Tokyo, Japan .
Zenyaku Kogyo (Japan) · JP

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The obstacles to the development of therapeutic aptamers for systemic inflammatory diseases, such as nuclease degradation and renal clearance, have not been fully overcome. Here, we report a novel PEGylation method, sbC-PEGylation, which improves the pharmacokinetic properties of RNA aptamers that act against interleukin-17A (IL-17A) in mice and monkeys. sbC-PEGylated aptamers were synthesized by coupling the symmetrical branching molecule 2-cyanoethyl-N,N-diisopropyl phosphoroamidite to the 5' end of the aptamer, before conjugating two polyethylene glycol (PEG) molecules to the aptamer. Pharmacokinetic studies showed that compared with conventionally PEGylated aptamers, the sbC-PEGylated aptamer exhibited excellent stability in the blood circulation of mice and monkeys. In addition, one of the sbC-PEGylated aptamers, 17M-382, inhibited the interleukin-6 (IL-6) production induced by IL-17A in NIH3T3 cells in a concentration-dependent manner, and the half-maximal inhibitory concentration of sbC-PEGylated 17M-382 was two times lower than that of non-PEGylated 17M-382. Furthermore, the intraperitoneal administration of sbC-PEGylated 17M-382 significantly inhibited the IL-6 production induced by IL-17A in a mouse air pouch model. Our findings suggest that the novel PEGylation method described in this study, sbC-PEGylation, could be used to develop anti-IL-17A aptamers as a therapeutic option for systemic inflammatory disease.

Indexed as

AnimalsAptamers, NucleotideBlood Chemical AnalysisHumansInhibitory Concentration 50Injections, IntraperitonealInterleukin-17Interleukin-6Interleukin-6 InhibitorsMacaca fascicularisMaleMiceMice, Inbred C57BLNIH 3T3 CellsPolyethylene GlycolsAptamers, NucleotideIL17A protein, humanInterleukin-17Interleukin-6Interleukin-6 Inhibitorsinterleukin-6, mousePolyethylene Glycolsaptamerinterleukin-17APEGylationpharmacokinetics

Identifiers

PMID27827561
PMCPMC5312557
OpenAlexW2562883104

What OpenQuestion holds

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LicenceCC BY
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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.